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. Androgen Receptor antagonist

    (R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells.
  2. Androgen antagonist

    17 alpha-propionate is a new topical and peripherally selective androgen antagonist.
  3. Androgen Receptor antagonist

    Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
  4. RAAS antagonist

    Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).
  5. Androgen receptor antagonist

    Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
  6. AT1 antagonist

    Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
  7. Androgen receptor antagonist

    MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.
  8. Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
  9. Angiotensin II receptor antagonist

    Tasosartan is an angiotensin II receptor antagonist.
  10. AT1 Antagonist

    Telmisartan is an angiotensin II receptor antagonist that inhibits the angiotensin II AT1 receptor.
  11. angiotensin II receptor antagonist

    Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
  12. AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
  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. AR antagonist

    RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
  15. CRTH2 antagonist

    OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist.
  16. 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.
  17. 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.
  18. 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.
  19. GnRH antagonist

    Abarelix acetate is a synthetic peptide gonadotropin releasing hormone receptor (GnRH) antagonist
  20. Estrogen receptor antagonist

    Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.
  21. GnRH antagonist

    Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist.
  22. CRTH2 receptor antagonist

    AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM.
  23. angiotensin AT2 receptor antagonist

    PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.
  24. ERRα antagonist/inverse agonist

    XCT 790 is a potent and specific inverse agonist of ERRα.
  25. Angiotensin AT1 receptor antagonist

    SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
  26. ETBR antagonist

    IRL-2500 is a potent, selective ETBR antagonist. It shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively).
  27. GnRH antagonist

    Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels.
  28. androgen-receptor (AR) antagonist

    N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors.
  29. progesterone receptor antagonist

    Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.
  30. angiotensin II receptor antagonist

    BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor.
  31. Glucocorticoid receptor antagonist

    The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.
  32. AT1 receptor antagonist

    EXP-3174 is a potent and selective noncompetitive AT1 receptor antagonist with IC50 value of 37 nM.
  33. EBI2 (GPR183) receptor antagonist

    NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).
  34. CRTH2 antagonist

    ACT-129968 is a potent and selective CRTH2 antagonist.
  35. Androgen receptor antagonist

    ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.
  36. Androgen Receptor antagonist

    EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ?? 6 μM)
  37. estrogen receptor downregulator and antagonist

    AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist.
  38. GPR139 antagonist

    NCRW0005-F05, first antagonist selective for GPR139 (IC50 value 0.21 uM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054.
  39. angiotensin II receptor type 1 antagonist

    Azilsartan medoxomil is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.
  40. Aldosterone Receptor Antagonist

    Esaxerenone, also known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid that acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.
  41. ER antagonist

    Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer.
  42. ERβ receptor antagonist

    PHTPP is a pyrazolo[1,5-α]pyrimidine-based ligand that acts as a full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα.
  43. Androgen receptor antagonist

    Spironolactone is a potent antagonist of the androgen receptor.
  44. non-peptide angiotensin II receptor antagonist

    Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys.
  45. Angiotensin II receptor antagonist

    Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
  46. GnRH antagonist

    Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.
  47. thromboxane A2 (TXA2) receptor (TP receptor) antagonist

    Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma.
  48. GnRH antagonist

    Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment. The IC50 of 1.21 nM.
  49. Glucocorticoid Receptor Antagonist

    OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM).
  50. CRTH2/DP2 receptor antagonist

    CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.

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