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  • Endocrinology-Hormones

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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Items 1-50 of 91

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Citations
  1. A13252
    GANT61

    GLI antagonist

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
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  2. A10905
    Telmisartan

    AT1 Antagonist

    Telmisartan is an angiotensin II receptor antagonist that inhibits the angiotensin II AT1 receptor.
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  3. A13201
    PD 123319 ditrifluoroacetate

    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.
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  4. A14130
    Lonaprisan

    progesterone receptor antagonist

    Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.
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  5. A12639
    Endoxifen (Z-isomer)

    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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  6. 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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  7. 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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  8. A10885
    Tamoxifen Citrate

    Estrogen receptor antagonist

    Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.
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  9. A15797
    Darolutamide (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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  10. A10562
    Enzalutamide (MDV3100)

    Androgen receptor antagonist

    MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.
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  11. A15451
    EXP-3174 (Losartan Carboxylic Acid)

    AT1 receptor antagonist

    EXP-3174 (Losartan Carboxylic Acid) is a potent and selective noncompetitive AT1 receptor antagonist with IC50 value of 37 nM.

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  12. 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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  13. A12312
    Ketodarolutamide (ORM-15341)

    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.
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  14. A12340
    GPR4 antagonist 1

    GPR4 antagonist

    GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.
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  15. A12350
    Ozarelix

    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.
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  16. A12613
    Abarelix

    GnRH antagonist

    Abarelix is a synthetic peptide gonadotropin releasing hormone receptor (GnRH) antagonist

     
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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. A13299
    XCT 790

    ERRα antagonist/inverse agonist

    XCT 790 is a potent and specific inverse agonist of ERRα.
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  19. A11121
    Eprosartan

    AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
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  20. 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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  21. A11445
    GW-1100

    GPR40 antagonist

    GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
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  22. A11541
    RU 58841

    AR antagonist

    RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
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  23. A12194
    AL082D06

    GR antagonist

    AL082D06 is a nonsteroidal glucocorticoid receptor antagonist.
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  24. A13591
    SL910102

    Angiotensin AT1 receptor antagonist

    SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
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  25. A13638
    IRL-2500

    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).
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  26. A13675
    G15

    GPER/GPR30 antagonist

    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
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  27. 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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  28. A13964
    N-desMethyl EnzalutaMide

    androgen-receptor (AR) antagonist

    N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors.
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  29. 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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  30. A14340
    RU43044

    Glucocorticoid receptor antagonist

    The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.
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  31. 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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  32. A17345
    Spironolactone

    Androgen receptor antagonist

    Spironolactone is a potent antagonist of the androgen receptor.
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  33. 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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  34. 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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  35. 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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  36. 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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  37. A18468
    OP-3633

    Glucocorticoid Receptor Antagonist

    OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM).
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  38. 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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  39. A20860
    Azilsartan medoxomil monopotassium

    angiotensin II receptor type 1 antagonist

    Azilsartan medoxomil monopotassium 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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  40. A20879
    Sparsentan

    angiotensin II and endothelin A receptor antagonist

    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
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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. A21466
    GLPG0974

    FFA2/GPR43 antagonist

    GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
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  44. A19586
    Proxalutamide

    AR antagonist

    Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.
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  45. A19587
    ORIC-101

    glucocorticoid receptor antagonist

    ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity.
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  46. A19630
    DC260126

    GPR40 antagonist

    DC260126, a small-molecule antagonist of GPR40.
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  47. A19747
    GDC-0927

    estrogen receptor antagonist

    GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
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  48. A19894
    MS21570

    GPR171 antagonist

    MS21570 is a selective GPR171 antagonist, with an IC50 of 220 nM.
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  49. A19919
    TR antagonist 1

    TR antagonist

    TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.
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  50. A19928
    GC 14

    thyroid hormone receptor antagonist

    GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
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