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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

Items 101-150 of 1456

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Catalog No.
Product Name
Application
Product Information
Citations
  1. A12311
    MK-6913

    Estrogen receptor β agonist

    Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
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  2. 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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  3. A12340
    GPR4 antagonist 1

    GPR4 antagonist

    GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.
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  4. 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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  5. A12375
    NBI-42902

    GnRH receptor Inhibitor

    NBI-42902 is a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor
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  6. A12376
    SR 144528

    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.
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  7. A12396
    AZD3514

    AR inhibitor downregulator

    AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.
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  8. A12462
    GPR35 agonist 1

    GPR35/CXCR8 agonist

    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
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  9. 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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  10. A12613
    Abarelix

    GnRH antagonist

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

     
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  11. A12629
    KW-8232 free base
    KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
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  12. A12634
    MBX-2982

    GPR119 agonist

    MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion.
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  13. 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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  14. A12645
    GSK-2881078

    androgen receptor modulator

    GSK-2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.
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  15. A12769
    Zofenopril calcium

    ACE inhibitor

    Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.
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  16. A12771
    Acolbifene (EM 652, SCH57068)

    estrogen receptor modulator

    acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).
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  17. A12790
    Parathyroid Hormone 1-34, Human
    Human parathyroid hormone (hPTH) peptide fragment; contains the 34 N-terminal residues of hPTH. Agonist at parathyroid 1 (PTH1) and parathyroid 2 (PTH2) receptors.
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  18. A12805
    BMS564929

    Androgen receptor (AR) modulator

    BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator, and this compound has been advanced to clinical trials for the treatment of age-related functional decline.
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  19. A12840
    Degarelix acetate

    GnRH antagonist

    Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist.
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  20. A12862
    Ganirelix acetate
    Ganirelix is an injectable competitive gonadotropin-releasing hormone antagonist (GnRH antagonist)
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  21. A12982
    MK-6892

    GPR109A agonist

    MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A.K i and GTPγS EC 50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
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  22. A12987
    Etersalate
    Etersalate inhibits platelet function and decreases thromboxane A2 (TXA2) levels.
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  23. A12994
    TUG-770

    FFA1/GPR40 Agonist

    TUG-770 is a Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
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  24. A13193
    SR1001

    ROR agonist

    SR1001 is a selective ROR-alpha and ROR-gamma inverse agonist; suppresses TH17 cell differentiation and inhibits autoimmunity.
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  25. 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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  26. A13215
    (Glp1)-Apelin-13

    Apelin Receptor activator

    (Glp1)-Apelin-13 is an activator of Apelin Receptor
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  27. A13248
    MGL-3196

    thyroid hormone receptor agonist

    MGL-3196 is an orally small-molecule liver-directed thyroid hormone receptor agonist designed to increase cholesterol uptake into the liver and increase its metabolism.
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  28. A13249
    AZD5423

    nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
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  29. 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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  30. A13292
    Arzoxifene HCl
    Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
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  31. A13299
    XCT 790

    ERRα antagonist/inverse agonist

    XCT 790 is a potent and specific inverse agonist of ERRα.
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  32. A13329
    Propyl pyrazole triol

    ERα agonist

    Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist.
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  33. A13359
    Diphenyleneiodonium chloride

    GPR3 agonist/NOS/ NADPH oxidases inhibitor

    Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells.
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  34. A13398
    Bopindolol malonate

    Bopindolol malonate is a non-selective, potent, long-acting beta adrenoceptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation.

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  35. A13464
    GHRP-6 Acetate
    GHRP-6 Acetate is a growth hormone releasing peptide.
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  36. A13468
    AMG 837 calcium hydrate

    GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
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  37. A13515
    TAK-700 Salt (Orteronel Salt)

    CYP17A1/androgen synthesis inhibitor

    Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
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  38. A13521
    Captopril disulfide

    LTA4 hydrolase inhibitor

    Captopril Disulfide is a reversible and competitive inhibitor of LTA4 hydrolase (IC50=11 M). Captopril has been shown to be an of angiotensin converting enzyme-1 (ACE1), but not ACE2(IC50 = 22 nM).
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  39. A13536
    AEZS-108

    GnRH-1 agonist

    AEZS-108 is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity.
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  40. A13568
    SR-2211

    RORr agonist

    SR-2211 selectively binds RORr(Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORr activity (IC50 = 320 nM).
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  41. A13591
    SL910102

    Angiotensin AT1 receptor antagonist

    SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
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  42. A13615
    Zofenopril

    ACE inhibitor

    Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
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  43. 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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  44. 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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  45. A13716
    AR-231453

    GPR119 agonist

    AR-231453 is a potent and selective small molecule agonis of GPR119 that enhances glucose dependent insulin secretion and glucagon like peptide-1 (GLP-1) release.
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  46. A13740
    Zearalenone
    Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
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  47. A13747
    Eprosartan mesylate
    Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 ?€? 3.9 nM and an elimination half-life of five to seven hours.
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  48. 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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  49. A13964
    N-desMethyl EnzalutaMide

    androgen-receptor (AR) antagonist

    N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors.
    Quick View
  50. A14024
    VTP-27999 HCl

    Renin inhibitor

    VTP-27999 HCl is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin.
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