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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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. angiotensin II receptor antagonist

    Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
  2. 5-alpha reductase inhibitor

    β-sitosterol reduces blood levels of cholesterol, and is sometimes used in treating hypercholesterolemia. β-Sitosterol inhibits cholesterol absorption in the intestine. When the sterol is absorbed in the intestine, it is transported by lipoproteins and incorporated into the cellular membrane.
  3. Aromatase inhibitor

    Fadrozole is a nonsteroidal aromatase inhibitor exhibiting a very potent and selective inhibitory effect of the aromatase enzyme system in vivo and estrogen biosynthesis in vivo.
  4. AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
  5. HMG-CoA reductase inhibitor

    Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease.
  6. renin inhibitor

    Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren, which is a direct renin inhibitor approved for the treatment of essential hypertension.
  7. CYP17 inhibitor

    TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
  8. HMG-CoA Reductase inhibitor

    Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.

  9. ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
  10. ACE inhibitor/Beta blocker

    Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction.
  11. Calcifediol-D6 is the deuterated form of Calcifediol(25-hydroxy Vitamin D3), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase.
  12. Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
  13. Androgen Receptor antagonist

    Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity.
  14. VD/VDR Inhibitor

    Metabolite of vitamin D2
  15. Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.
  16. Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
  17. AR antagonist

    RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
  18. Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.
  19. Renin inhibitor

    VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases. Ic50 value: Target: Renin
  20. Olmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion.
  21. Renin inhibitor

    Aliskiren is an orally active, synthetic nonpeptide renin inhibitor.
  22. progesterone receptor agonist

    Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
  23. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
  24. Ethisterone is a progestogen hormone.
  25. Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.
  26. Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
  27. Meclizine is a human pregnane X receptor (hPXR) agonist. It possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible.
  28. Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I.
  29. Captopril is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure.
  30. Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme inhibitor (ACE) which is used for the treatment of hypertension and congestive heart failure.
  31. ACE inhibitor

    Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure.
  32. ACE inhibitor

    Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure.
  33. ACE inhibitor

    Temocapril is an ACE inhibitor.
  34. AT1 Receptor Blocker

    Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension.
  35. estrogen agonist

    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
  36. Fluticasone propionate is a high affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM).
  37. Imidapril (Tanatril) is an inhibitor of angiotensin converting enzyme (ACE).
  38. Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
  39. Pregnenolone is an endogenous steroid hormone for inhibition of M1 receptor- and M3 receptor-mediated currents with IC50 of 11.4 μM and 6.0 μM, respectively.
  40. CRTH2 antagonist

    OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist.
  41. Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
  42. Impurity of Doxercalciferol is an impurity of doxercalciferol, which is a synthetic analog of ergocalciferol (vitamin D2), used as a drug for secondary hyperparathyroidism and metabolic bone disease, and it suppresses parathyroid synthesis and secretion.
  43. Estrogen receptor degrader

    Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  44. Estrogen receptor β agonist

    Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
  45. human AR (hAR) antagonist

    ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
  46. GnRH antagonist

    Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors.
  47. GnRH receptor Inhibitor

    NBI-42902 is a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor
  48. CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
  49. AR inhibitor downregulator

    AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.
  50. Estrogen receptor antagonist

    (E/Z)-4-hydroxy Tamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.

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