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
Citations
  1. 5 alpha-reductase inhibitor

    Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.
  2. gonadotropin-releasing hormone agonist

    Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).
  3. TRH-R agonist

    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).
  4. Flurandrenolide is a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Flurandrenolide exerts its effects by interacting with specific cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression.
  5. 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.
  6. FFA4/GPR120 agonist

    TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism.
  7. Glucocorticoid receptor agonist

    GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.
  8. RORγ inverse agonist

    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
  9. OC2 inhibitor

    CSRM617 is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.

  10. glucocorticoid receptor agonist

    Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.
  11. Glucocorticoid Receptor Antagonist

    OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM).
  12. aromatase inhibitor

    Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
  13. PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  14. ROR agonist

    ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5.
  15. 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.
  16. glucocorticoid

    Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.
  17. RORγ agonist

    AZD-0284 is a potent, selective, inverse agonist of the nuclear receptor RORγ for the potential treatment of Plaque psoriasis.
  18. 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.
  19. 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.
  20. selective glucocorticoid receptor modulator

    AZD9567 is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM.
  21. GPRC6A agonist

    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  22. ACE inhibitor

    H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
  23. GPR27 agonist

    CID 1375606 is a GPR27 agonist.
  24. ERRa degrader

    PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
  25. ERRα Degrader

    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
  26. glucocorticoid receptor agonist

    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively.
  27. ERRα inverse agonist

    PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
  28. Progesterone receptor modulator

    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  29. apelin agonist

    Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions.
  30. RORγt inverse agonist

    A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release.
  31. Androgen metabolite

    Beta-Cortol is an androgen metabolite present in adults.
  32. Deoxycorticosterone is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as an aldosterone precursor.
  33. CX3CR1 antagonist

    JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM.
  34. RORγt inhibitor

    S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production.
  35. 3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M-1 for TRα1 and TRβ1, respectively.
  36. hGPR91 antagonist

    HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM.
  37. GPR40 full agonist

    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  38. GPR52 agonist

    FTBMT is a selective GPR52 agonist with an EC50 of 75 nM. Antipsychotic and procognitive properties.
  39. GPR4 antagonist

    NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.
  40. full progesterone receptor agonist

    Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
  41. GPR120 agonist

    GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
  42. GPR139 agonist

    TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
  43. G-1

    GPR30 agonist

    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
  44. GPR119 agonist

    Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
  45. ERRγ agonist

    GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
  46. apelin receptor agonist

    MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart.
  47. 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.
  48. PGI2 receptor agonist and vasodilator

    Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
  49. 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.
  50. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

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