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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 51-91 of 91

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  1. A19950
    RTI-13951-33

    brain-penetrant GPR88 agonist

    RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay.
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  2. A19953
    ML 145

    GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
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  3. A19960
    H3B-5942

    estrogen receptor covalent antagonist

    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively.
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  4. 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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  5. A20100
    H3B-6545

    Estrogen receptor antagonist

    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
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  6. A20193
    GPR84 antagonist 8

    GPR84 antagonist

    GPR84 antagonist 8 is a selective GPR84 antagonist.
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  7. A20203
    UT-155

    AR antagonist

    UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
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  8. A20417
    Nitromifene

    ER antagonist

    Nitromifene is an antagonist of estrogen receptor (ER).
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  9. 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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  10. A18767
    (E)-GW7604

    EStrogen receptor (ER) antagonist

    GW7604 is an antiestrogen agbent, and is tthe presumed metabolite of GW5638 in breast (MCF-7) and endometrial (ECC-1) cell lines in vitro.
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  11. 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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  12. A19100
    JMS-17-2

    CX3CR1 antagonist

    JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM.
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  13. A19155
    hGPR91 antagonist 1

    hGPR91 antagonist

    HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM.
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  14. A19231
    NE 52-QQ57

    GPR4 antagonist

    NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.
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  15. 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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  16. A19480
    Apararenone

    mineralocorticoid receptor antagonist

    Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
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  17. 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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  18. 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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  19. A16818
    CID16020046

    GPR55 antagonist

    CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
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  20. A16925
    Esaxerenone

    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.
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  21. A16994
    Fulvestrant S enantiomer

    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.
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  22. A15775
    NIBR189

    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).
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  23. 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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  24. A15822
    AZD9496

    estrogen receptor downregulator and antagonist

    AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist.
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  25. 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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  26. A10009
    17 alpha-propionate

    Androgen antagonist

    17 alpha-propionate is a new topical and peripherally selective androgen antagonist.
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  27. 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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  28. A10477
    Irbesartan (Avapro)

    AT1 antagonist

    Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
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  29. A10891
    Tasosartan

    Angiotensin II receptor antagonist

    Tasosartan is an angiotensin II receptor antagonist.
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  30. 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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  31. A21545
    Fulvestrant R enantiomer

    estrogen receptor antagonist

    Fulvestrant R enantiomer (ICI 182780 R enantiomer; ZD 9238 R enantiomer; ZM 182780 R enantiomer) is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.
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  32. A21578
    Losartan (D4 Carboxylic Acid)

    angiotensin II receptor antagonist

    Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist.
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  33. A21600
    Azilsartan D5

    angiotensin II type 1 receptor antagonist

    Azilsartan D5 is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist.
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  34. A21629
    H3B-6545 Hydrochloride

    estrogen receptor covalent antagonist

    H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).
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  35. 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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  36. A21830
    Enclomiphene citrate

    oestrogen receptor antagonist

    Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
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  37. 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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  38. 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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  39. 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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  40. 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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  41. A84995
    AR antagonist 4

    AR Antagonist/Degrader

    AR Antagonist 4 is a potent orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wild-type AR. In addition to its antagonistic properties, it functions as an AR degrader with a DC50 of 2.84 μM. This dual activity positions AR Antagonist 4 as a valuable tool in research related to androgen signaling, hormone-dependent cancers, and potential therapeutic approaches targeting the AR pathway.
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