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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

Diabetes Research

Endocrinology Research Products

Kisspeptin Receptor

Leptin Receptors

Melanocortin (MC) Receptors

Mineralocorticoid Receptors

Galanin Receptors

TRH Receptors

Ghrelin Receptors

Natriuretic Peptide Receptors

NPY Receptors

Motilin Receptor

PTH Receptor

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49 Items

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. A10008
    (R)-Bicalutamide

    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.
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  2. A10009
    17 alpha-propionate

    Androgen antagonist

    17 alpha-propionate is a new topical and peripherally selective androgen antagonist.
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  3. A10142
    Bicalutamide (Casodex)

    Androgen Receptor antagonist

    Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
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  4. A10175
    Candesartan (Atacand)

    RAAS antagonist

    Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).
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  5. A10402
    Flutamide

    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.
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  6. A10477
    Irbesartan (Avapro)

    AT1 antagonist

    Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
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  7. A10562
    MDV3100

    Androgen receptor antagonist

    MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.
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  8. A10885
    Tamoxifen Citrate

    Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
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  9. A10905
    Telmisartan

    AT1 Antagonist

    Telmisartan is an angiotensin II receptor antagonist that inhibits the angiotensin II AT1 receptor.
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  10. A10962
    Valsartan

    angiotensin II receptor antagonist

    Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
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  11. A11121
    Eprosartan

    AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
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  12. A11409
    Cyproterone acetate

    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.
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  13. A11541
    RU 58841

    AR antagonist

    RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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  14. A11946
    OC 000459

    CRTH2 antagonist

    OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist.
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  15. A12532
    (E/Z)-4-hydroxy Tamoxifen

    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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  16. A12639
    Endoxifen

    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.
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  17. A12840
    Degarelix acetate

    GnRH antagonist

    Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist.
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  18. A13186
    AZD1981

    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.
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  19. A13299
    XCT 790

    ERRα antagonist/inverse agonist

    XCT 790 is a potent and specific inverse agonist of ERRα.
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  20. A13893
    Elagolix sodium

    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.
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  21. A14154
    BIBS39

    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.
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  22. A15451
    EXP-3174

    AT1 receptor antagonist

    EXP-3174 is a potent and selective noncompetitive AT1 receptor antagonist with IC50 value of 37 nM.
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  23. A15780
    ACT-129968 (Setipiprant)

    CRTH2 antagonist

    ACT-129968 is a potent and selective CRTH2 antagonist.
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  24. A15797
    ODM-201

    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.
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  25. A15814
    EPI-001

    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)
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  26. A16184
    NCRW0005-F05

    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.
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  27. A16420
    Azilsartan Medoxomil

    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.
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  28. A17035
    PHTPP

    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.
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  29. A17345
    Spironolactone

    Androgen receptor antagonist

    Spironolactone is a potent antagonist of the androgen receptor.
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  30. A17477
    Fimasartan

    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.
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  31. A17510
    Losartan

    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.
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  32. A17783
    Relugolix

    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.
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  33. A18134
    Seratrodast

    thromboxane A2 (TXA2) receptor (TP receptor) antagonist

    Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma.
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  34. A18282
    Cetrorelix Acetate

    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.
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  35. A18620
    Exicorilant

    Glucocorticoid receptor (GR) antagonist

    Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia.
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  36. A18799
    ML401

    EBI2 (GPR183) antagonist

    ML401 is an antagonist of the EBI2 receptor with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity.
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  37. A19446
    ML221

    APJ functional antagonist

    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
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  38. A19894
    MS21570

    GPR171 antagonist

    MS21570 is a selective GPR171 antagonist, with an IC50 of 220 nM.
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  39. A19987
    D4-abiraterone

    androgen receptor antagonist

    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
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  40. A20589
    Sufugolix

    LHRH receptor antagonist

    Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
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  41. A21165
    Nilutamide

    Androgen receptor antagonist

    Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma.
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  42. A21184
    (R)-Elagolix

    GnRHR antagonist

    Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
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  43. A21612
    AM211

    PGD2) receptor type 2 (DP2) antagonist

    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
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  44. A21726
    AZD9496 maleate

    estrogen receptor (ERα) antagonist

    AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
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  45. A21830
    Enclomiphene citrate

    oestrogen receptor antagonist

    Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
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  46. A21883
    Timapiprant sodium

    D prostanoid receptor 2 antagonist

    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist.
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  47. A22088
    ML191

    GPR55 antagonist

    ML191 (CCG-152883, CID-23612552) is an antagonist of GPR55 with EC50 of 1.076 ?M in U2OS cells overexpressing GPR55.
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  48. A22553
    ML-193

    GPR55 antagonist

    ML 193 is a selective GPR55 antagonist (IC50 = 221 nM). Exhibits >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively. Inhibits ERK signaling in vitro.
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  49. A22622
    Cetrorelix diacetate

    GnRH receptor antagonist

    Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
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