Endocrinology-Hormones

Small molecules play a pivotal role in Endocrinology Research. These are low molecular weight compounds that have a significant impact on the endocrine system, hormones, and their receptors. Here are some key aspects of how small molecules are involved in this field:

  • Hormone Mimetics and Inhibitors: Small molecules are used to develop synthetic compounds that mimic the actions of hormones or inhibit their effects. For example, drugs like metformin for diabetes management and selective estrogen receptor modulators (SERMs) for breast cancer treatment are used to either mimic or block hormonal activity.
  • Receptor Modulation: Small molecules can bind to hormone receptors and modulate their activity. This is crucial in developing drugs that target specific hormone receptors, like the use of small molecule agonists and antagonists to regulate thyroid hormone receptors.
  • Metabolism Regulation: Endocrinology research often focuses on metabolism and how hormones like insulin regulate it. Small molecules are employed to understand and develop drugs targeting enzymes involved in metabolism, such as glucagon-like peptide-1 (GLP-1) agonists for diabetes treatment.
  • Steroid Hormone Production: Small molecules may be utilized to influence the production of steroid hormones in the adrenal glands or gonads. This is essential for conditions like Cushing's syndrome or polycystic ovary syndrome (PCOS).
  • Hormone Assays: In laboratory research, small molecules are used as tracers or markers in hormone assays. For instance, small molecule fluorophores can be attached to antibodies to detect hormone levels in blood samples.

Drug Development: Endocrinology research relies on small molecules as potential drug candidates. Researchers design and test small molecules for their effectiveness in modulating hormonal pathways, with the goal of developing new therapies for endocrine disorders.
In summary, small molecules are indispensable tools in Endocrinology Research, enabling scientists to better understand the endocrine system's intricacies and develop novel treatments for a wide range of hormonal disorders and conditions. Their versatility and specificity make them valuable assets in advancing our knowledge of endocrinology and improving patient care.


Endocrinology Disease Products


Endocrinology Research Products

Kisspeptin Receptor

Leptin Receptors

Melanocortin (MC) Receptors

Mineralocorticoid Receptors

Ghrelin Receptors

Natriuretic Peptide Receptors

NPY Receptors

Motilin Receptor

PTH Receptor

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Citations
  1. 5α-Reductase Inhibitor

    Lapisteride is a potent 5α-reductase inhibitor, demonstrating efficacy in the modulation of androgen metabolism. This compound effectively inhibits 5α-reductase activity within hair follicles, making it a valuable tool for investigating prostatic hyperplasia and androgenic alopecia. Its applications extend to research aimed at understanding androgen-related disorders and developing targeted therapies.
  2. 5-Alpha Reductase Inhibitor

    CGP-53153 is a steroidal inhibitor of 5-alpha reductase, exhibiting IC50 values of 36 nM in rat prostatic tissue and 262 nM in human prostatic tissue. This compound is primarily utilized in research to investigate the inhibition of 5-alpha reductase, which plays a crucial role in androgen metabolism. Its biological activity makes it a valuable tool for studying conditions related to androgen levels, such as benign prostatic hyperplasia and prostate cancer.
  3. 5α-Reductase Inhibitor

    Izonsteride is a potent inhibitor of 5α-reductase, demonstrating IC50 values of 11.6 nM for type I and 7.37 nM for type II isoforms. By hindering the enzyme responsible for converting testosterone to dihydrotestosterone, Izonsteride effectively reduces androgenic activity. This compound has been shown to significantly inhibit the growth of LNCaP tumors in thymic mice, indicating its potential as a therapeutic agent in prostate cancer research, with minimal host toxicity observed.
  4. 5 alpha Reductase Inhibitor

    MK 386 is a selective inhibitor of 5-alpha reductase type I, which plays a critical role in the metabolism of testosterone into dihydrotestosterone (DHT). By inhibiting this enzyme, MK 386 is utilized in research focused on prostate cancer treatment and hormone-related disorders. Its specificity for 5-alpha reductase I makes it a valuable tool for studying the effects of DHT modulation on cellular and molecular pathways associated with prostate cancer progression.
  5. Steroid 5α-Reductase Inhibitor

    8,11-Eicosadiynoic acid is a steroid 5α-reductase inhibitor that exhibits potent biological activity in the modulation of androgen metabolism. This unsaturated fatty acid is primarily utilized in research related to acne and other androgen-mediated conditions. Its ability to inhibit 5α-reductase makes it a valuable tool for investigating pathways involved in sebaceous gland function and acne pathology.
  6. 5α-reductase Inhibitor

    Bexlosteride is a benzoquinolinone that acts as a specific inhibitor of human type I 5α-reductase. It exhibits significant metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. This compound is valuable for research focused on prostate cancer, providing insights into the modulation of androgen pathways and potential therapeutic interventions.
  7. 5alpha-reductase 1 Inhibitor

    AS-601811 is a potent inhibitor of 5α-reductase 1, demonstrating an IC50 of 20 nM. This compound is valuable for investigating conditions such as alopecia and hirsutism by modulating androgen metabolism. Its specificity for 5α-reductase 1 makes it an essential tool for research into related endocrine and dermatological disorders.
  8. 5 alpha Reductase Inhibitor

    ONO-3805 is a non-steroidal 5α-reductase inhibitor that selectively targets the enzyme responsible for converting testosterone to dihydrotestosterone. It exhibits potential therapeutic benefits in the management of benign prostatic hyperplasia and may contribute to the reduction of associated symptoms. This compound is primarily utilized in endocrine-related research and studies focusing on androgen modulation in prostatic disorders.
  9. Human Type I 5α-Reductase Inhibitor

    LY191704 is a selective, nonsteroidal inhibitor of human type I 5α-reductase, exhibiting noncompetitive inhibition. This compound, a racemic mixture of LY300502 and LY300503, demonstrates potent activity in modulating the enzymatic conversion of testosterone to dihydrotestosterone (DHT). LY191704 is valuable for investigating human endocrine disorders linked to elevated DHT levels, offering insights into potential therapeutic approaches for conditions such as androgenetic alopecia and benign prostatic hyperplasia.
  10. 5 alpha Reductase Inhibitor

    L-751788 is a selective inhibitor of type I 5α-reductase, a key enzyme involved in steroid metabolism. This compound demonstrates significant potential in reducing dihydrotestosterone levels without adversely affecting fetal external genitalia, as evidenced by studies conducted in pregnant rhesus monkeys. L-751788 is valuable for research applications investigating disorders of androgen metabolism and related therapeutic interventions.
  11. 5a-reductase Inhibitor

    (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is a potent inhibitor of 5α-reductase, exhibiting an IC50 value of 41.9 μM. This compound effectively inhibits testosterone-induced growth in the ventral prostate of rat models. It holds potential for research applications focused on benign prostatic hyperplasia (BPH) and other conditions linked to 5α-dihydrotestosterone (DHT), including acne and male pattern baldness.
  12. 5 alpha-Reductase Inhibitor

    Turosteride is a selective inhibitor of 5 alpha-reductase, demonstrating IC50 values of 55 nM and 53 nM for human and rat prostatic enzymes, respectively. This compound effectively reduces prostate and seminal vesicle weights, making it valuable in research related to benign prostatic hyperplasia and androgenic activity modulation. Turosteride can be instrumental in studies investigating the role of 5 alpha-reductase in prostatic diseases and hormone regulation.
  13. Steroid 5α-Reductase Inhibitor

    MK-0434 is an orally active inhibitor of steroid 5α-reductase, acting primarily to inhibit the conversion of testosterone into dihydrotestosterone (DHT). By reducing DHT levels, MK-0434 plays a significant role in the investigation of benign prostatic hyperplasia and other androgen-mediated conditions. This compound serves as a useful tool for researchers studying the hormonal pathways involved in prostate health and related disorders.
  14. 5α-reductase Inhibitor

    MK-0963 is a steroidal inhibitor of 5α-reductase, effectively reducing serum dihydrotestosterone (DHT) levels in a dose-dependent manner. This compound is valuable for studying dihydrotestosterone-related conditions, including benign prostatic hyperplasia (BPH). Its ability to modulate DHT concentrations makes MK-0963 a significant tool in research aimed at understanding and treating disorders associated with androgen metabolism.
  15. 5α-Reductase Inhibitor

    FR-146687 is a selective and orally bioavailable inhibitor of 5α-reductase, demonstrating IC50 values of 1.7 nM and 4.6 nM for rat and human enzymes, respectively. This compound exhibits specific inhibitory activity without affecting other steroid oxidoreductases. FR-146687 is utilized in research focused on disorders related to androgen metabolism and can aid in the development of therapeutic interventions targeting 5α-reductase-related pathways.
  16. 5 alpha Reductase Inhibitor

    5α-reductase-IN-1 is a potent inhibitor of 5α-reductase, an enzyme implicated in androgen metabolism. This compound is primarily utilized in research focused on androgenetic alopecia and may be investigated in conjunction with minoxidil to explore synergistic effects in hair regrowth studies. Its role in modulating testosterone derivatives offers valuable insights into potential therapeutic strategies for hair loss disorders.
  17. GPR88 Inhibitor

    GPR88-IN-1 is a selective inhibitor of GPR88, a G protein-coupled receptor involved in modulating dopaminergic signaling. This compound demonstrates potential for investigating the role of GPR88 in various central nervous system disorders, including schizophrenia and drug addiction. It serves as a valuable tool for researchers exploring therapeutic pathways related to neuropsychiatric conditions.
  18. angiotensin-converting enzyme Inhibitor, renin Inhibitor

    Lyciumin D functions as both an angiotensin-converting enzyme inhibitor and a renin inhibitor. This compound demonstrates significant potential in the modulation of the renin-angiotensin system, making it a valuable tool for research into hypertension and related cardiovascular conditions. Its multimodal mechanism can facilitate studies aimed at understanding blood pressure regulation and developing therapeutic strategies for hypertension management.
  19. Renin Inhibitor

    Imarikiren hydrochloride is a potent renin inhibitor that disrupts the renin-angiotensin (RA) system. This compound demonstrates significant biological activity in the context of cardiovascular and renal diseases, making it valuable for research related to hypertension, heart failure, and diabetic nephropathy. Its mechanism of action provides insights into the modulation of blood pressure and kidney function, facilitating the exploration of therapeutic strategies for these conditions.
  20. Renin Inhibitor

    SQ 33800 is a highly potent inhibitor of human renin, exhibiting an IC50 value of 0.35 nM. This compound is instrumental in the study of cardiovascular diseases, providing insights into the regulation of blood pressure and fluid balance. Researchers can utilize SQ 33800 to explore the implications of renin inhibition in various cardiovascular-related conditions.
  21. Direct Renin Inhibitor

    SPH3127 is a highly potent and orally active direct renin inhibitor, demonstrating an IC50 of 0.4 nM against recombinant human renin and 0.45 nM for human plasma renin activity. This compound exhibits significant antihypertensive properties, making it a valuable tool for research focused on essential hypertension and related cardiovascular studies. Its mechanism of action as a direct renin inhibitor allows for detailed investigation into the renin-angiotensin-aldosterone system and its implications in hypertension management.
  22. Renin Inhibitor

    Zankiren is a selective renin inhibitor that reduces the formation of angiotensin II, leading to its renal vasodilator effects. This compound is valuable for research focused on hypertension and cardiovascular diseases, as it specifically modulates renal hemodynamics without interfering with other vasodilatory pathways. Its ability to target renin makes Zankiren an important tool for studying the renin-angiotensin system and its implications in various pathological conditions.
  23. Renin Inhibitor

    SQ 32970 is a tripeptidic inhibitor targeting renin, a key enzyme in the regulation of blood pressure. This compound exhibits potent inhibition of endothia protease activity, making it valuable for studies related to hypertension and cardiovascular research. SQ 32970 serves as a useful tool for investigating the physiological and pathological roles of the renin-angiotensin system.
  24. Renin Inhibitor

    SQ 31844 is a novel renin inhibitor from the imidazolidinol class, specifically targeting the enzyme renin. This compound demonstrates potent in vitro inhibition of primate renin while showing no significant effects on renin from rat, pig, or dog. In vivo studies in sodium-deprived cynomolgus monkeys reveal a dose-dependent reduction in plasma renin activity (PRA) and arterial blood pressure, particularly at higher intravenous doses. Notably, oral administration of SQ 31844 at 50 μmol/kg leads to an 80% reduction in PRA. SQ 31844 serves as a valuable tool for exploring renin-related cardiovascular research and hypertension studies.
  25. Renin Inhibitor

    Renin IN-2 is a selective inhibitor of human renin, exhibiting an IC50 value of 0.059 μM. This compound demonstrates oral efficacy and is applicable in the study of hypertension. Research utilizing Renin IN-2 can provide insights into renin's role in the regulation of blood pressure and related cardiovascular conditions.
  26. Renin Inhibitor

    Renin-IN-4 is a potent renin inhibitor that modulates the renin-angiotensin system. This compound is primarily studied for its implications in cardiovascular diseases, as it plays a crucial role in regulating blood pressure and fluid balance. Renin-IN-4 serves as a valuable tool for investigating the pathophysiology of hypertension and related cardiovascular disorders.
  27. Renin Inhibitor

    Ciprokiren is a potent renin inhibitor, exhibiting IC50 values of 0.07 nM in buffer and 0.65 nM in plasma. This compound can be applied transdermally while maintaining hemodynamic effects without reducing plasma renin activity or plasma immunoreactive angiotensin II levels. Ciprokiren demonstrates significant antihypertensive efficacy, making it a valuable tool for hypertension research and the study of renin-angiotensin system modulation.
  28. Renin Inhibitor

    CGP 29287 is a potent inhibitor of renin, the enzyme responsible for the conversion of angiotensinogen to angiotensin I in the renin-angiotensin system. By selectively inhibiting renin activity, CGP 29287 plays a critical role in studying the regulation of blood pressure and cardiovascular function. This compound is useful in research applications focusing on hypertension, heart failure, and related metabolic disorders.
  29. Renin Inhibitor

    CP-85339 is a tetrapeptide compound that functions as a selective renin inhibitor, effectively modulating the renin-angiotensin-aldosterone system. It demonstrates significant biological activity by decreasing plasma renin levels, which can contribute to lowering blood pressure. This reagent is utilized in research applications related to cardiovascular diseases and hypertension studies, providing insights into the therapeutic potential of renin inhibition.
  30. Renin Inhibitor

    SQ 30774 is a selective renin inhibitor that demonstrates potent in vitro activity in primate models. This compound effectively reduces plasma renin activity (PRA) and has been shown to lower arterial blood pressure in vivo. SQ 30774 is valuable for research applications focusing on hypertension and the renin-angiotensin system, providing insights into cardiovascular regulation and potential therapeutic interventions.
  31. Renin Inhibitor

    Terlakiren is an orally active renin inhibitor that effectively modulates blood pressure regulation. With an IC50 value of 0.7 nM against human renin, Terlakiren demonstrates potent inhibition, making it a valuable tool for studying hypertension and related cardiovascular conditions. This compound is useful in research focused on renin-angiotensin system modulation and potential therapeutic interventions for hypertension.
  32. Renin Inhibitor

    L-363564 is a potent renin inhibitor that plays a critical role in the modulation of the renin-angiotensin-aldosterone system (RAAS). This compound is primarily utilized in cardiovascular disease research, aiding in the investigation of hypertension and related conditions. Its ability to effectively inhibit renin activity makes it a valuable tool for exploring therapeutic strategies in this area.
  33. Renin Inhibitor

    CGP 44099 is a selective renin inhibitor that plays a critical role in the modulation of the renin-angiotensin system. This compound is particularly valuable for research on ischemic injury and the mechanisms underlying reperfusion arrhythmias in rat heart models, providing insights into cardiovascular pathophysiology and potential therapeutic interventions.
  34. Renin inhibitor

    SR 42128 is a potent renin inhibitor that primarily targets the renin-angiotensin system. This compound demonstrates significant inhibition of primate renin activity, while exhibiting reduced efficacy against renins from other species. SR 42128 is valuable for research applications focused on hypertension, cardiovascular disease, and renal function studies.
  35. Renin Inhibitor

    Ditekiren is a pseudohexapeptide renin inhibitor that targets the renin-angiotensin system. It effectively inhibits renin activity, leading to a reduction in the formation of angiotensin II, a key vasoconstrictor involved in blood pressure regulation. This compound is valuable for research applications focused on hypertension, cardiovascular physiology, and fluid balance studies.
  36. Renin Inhibitor

    U-80125 is a competitive inhibitor of human renin, demonstrating an IC50 value of 2.3 μM. This dansylated peptide is characterized by excitation and emission maxima at 340 and 530 nm, respectively. U-80125 is valuable for research focused on hypertension and cardiovascular disease, facilitating the study of renin's role in the renin-angiotensin-aldosterone system.
  37. Renin Inhibitor

    MK-8141 (ACT-077825) is a selective renin inhibitor that increases immunoreactive renin (ir-AR) levels by up to sevenfold. Its primary research applications are focused on evaluating antihypertensive efficacy in hypertensive models. Although MK-8141 demonstrates changes in ir-AR, it does not result in sustained reductions in plasma renin activity (PRA) and does not produce significant blood pressure-lowering effects.
  38. Renin Inhibitor

    Renin-IN-3 is a potent renin inhibitor that selectively targets the renin-angiotensin system. It has demonstrated significant biological activity in modulating blood pressure, making it a valuable tool for hypertension research. This compound can be utilized to explore mechanisms of renal function and cardiovascular regulation in various experimental models.
  39. Renin Inhibitor/Microbiota Modulator

    Theasinensin C is an orally active renin inhibitor with an IC50 of 40.21 μM, demonstrating significant modulation of gut microbiota. It selectively enhances the population of Akkermansia muciniphila, promoting beneficial hydrolysis of mucin and influencing the gut-kidney-liver metabolic signaling pathways that contribute to creatine biosynthesis. This compound is valuable for studying hypertension and neuroinflammation, especially in the context of high-fructose diets, as it has been shown to improve cognitive function, reduce pro-inflammatory cytokines, and restore intestinal barrier integrity.
  40. Renin Inhibitor

    PD 132002 is a potent, orally active inhibitor of renin, a key enzyme in the renin-angiotensin system. By effectively reducing plasma renin activity, PD 132002 leads to significant decreases in blood pressure. This compound serves as a valuable tool for research into hypertension and related cardiovascular disorders. Additionally, it exhibits weak inhibition of pepsin, highlighting its specific targeting mechanism.
  41. Renin Inhibitor

    CP 71362 is a potent renin inhibitor that acts as a substrate-analog transition state mimic, demonstrating significant antihypertensive activity. It effectively inhibits plasma renin across species, with IC50 values of 3 nM in rats, 0.0033 nM in dogs, and 20 nM in humans. CP 71362 significantly reduces mean arterial pressure in both anesthetized and conscious sodium-depleted models, showing a dose-dependent effect. This compound is valuable for research focused on hypertension and congestive heart failure.
  42. Renin Inhibitor

    A-74273 is an orally active peptide renin inhibitor with an IC50 value of 3.1 nM. This compound competitively inhibits renin by binding to its active site, thereby obstructing the conversion of angiotensinogen to angiotensin I and subsequently reducing angiotensin II levels. A-74273 is utilized in research focused on hypertension and related cardiovascular diseases.
  43. Renin Inhibitor

    Renin inhibitor-1 is a potent, orally active renin inhibitor with IC50 values of 0.9 nM for recombinant human renin and 1.8 nM for human plasma renin activity (hPRA). This compound demonstrates significant antihypertensive efficacy, making it a valuable tool for studying hypertension and related cardiovascular and renal diseases. Its ability to effectively inhibit renin positions it as a key agent in cardiovascular research.
  44. Oligopeptide Renin Inhibitor

    PD 125967 is an oligopeptide renin inhibitor that specifically targets the renin-angiotensin system. It exhibits significant activity in lowering blood pressure, making it a valuable tool for cardiovascular research. This compound is useful for studying hypertension and related disorders, providing insights into the regulation of blood pressure through renin inhibition.
  45. Renin Inhibitor

    Remikiren is a potent and selective inhibitor of renin, demonstrating high specificity with IC50 values of 0.7 nM for human renin and 0.8 nM for human plasma renin. This compound effectively lowers mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys, making it a valuable tool for research into hypertension. Remikiren serves as a key reagent for exploring the renin-angiotensin system and its implications in cardiovascular diseases.
  46. Renin Inhibitor

    SR 43845 is a selective renin inhibitor that effectively reduces blood pressure by inhibiting plasma renin activity. This compound is primarily used in hypertension research, providing valuable insights into the regulation of blood pressure and the renin-angiotensin system. Its application in preclinical studies can aid in the development of therapeutic strategies for hypertension management.
  47. Renin Inhibitor

    PD-134672 is a potent renin inhibitor featuring a 2-amino-4-thiazolyl substituent. It demonstrates significant in vitro inhibition of monkey renin, while exhibiting only minimal effects on the related protease bovine feline hepsin D. This compound has shown oral hypotensive activity in hyperreninemic normotensive monkeys and has been identified for further evaluation in renal hypertensive models due to its strong efficacy and prolonged effects. PD-134672 is a valuable tool for research exploring mechanisms of hypertension and the therapeutic potential of renin inhibition.
  48. Renin Inhibitor

    EMD 52297 is a potent renin inhibitor that effectively modulates hemodynamic and hormonal responses. In addition to its primary action, EMD 52297 also exhibits activity as an angiotensin-converting enzyme (ACE) inhibitor. This compound is primarily utilized in cardiovascular research and hypertension studies, providing insights into the regulation of blood pressure and renal function.
  49. Renin Inhibitor

    A-65317 is a primate-selective renin inhibitor that exhibits a potent inhibitory effect with an IC50 of 0.37 nM. This compound is known for its long-lasting hypotensive response, making it valuable in cardiovascular research. A-65317 can be utilized in studies focused on hypertension and renal function regulation.
  50. Renin Inhibitor

    Cgp 38560 methanesulfonate is a selective renin inhibitor that modulates the renin-angiotensin system. This compound exhibits a dose-dependent decrease in angiotensin II levels and plasma renin activity, while simultaneously increasing active renin concentrations. Cgp 38560 methanesulfonate is utilized in research focused on hypertension and cardiovascular disease, providing valuable insight into renin regulation and therapeutic interventions.

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