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

Items 351-400 of 1754

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Catalog No.
Product Name
Application
Product Information
Citations
  1. selective estrogen receptor modulator (SERM)

    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
  2. Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement.
  3. 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.
  4. RORγ agonist

    LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist.
  5. androgen receptor modulator (SARM)

    LY2452473 is an orally bioavailable selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity.
  6. ACE2 inhibitor

    MLN-4760 is an angiotensin-converting (ACE2) inhibitor. In huMNCs, MLN-4760-B detected 63% ACE2 with 28-fold selectivity over ACE.
  7. 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.
  8. RORγt inhibitor

    AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.
  9. synthetic glucocorticoid receptor agonist

    Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
  10. 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.
  11. FAA1 agonist

    FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
  12. 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.
  13. AR antagonist

    Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.
  14. glucocorticoid receptor antagonist

    ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity.
  15. RORγt inverse agonist

    PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity.
  16. RORγt inverse agonist

    TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM).
  17. GPR40 antagonist

    DC260126, a small-molecule antagonist of GPR40.
  18. GPR68 modulator

    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83.
  19. GPR120 agonist

    GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.
  20. androgen ligand

    Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
  21. Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor.
  22. estrogen receptor degrader

    LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.
  23. estrogen ligand

    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
  24. estrogen receptor antagonist

    GDC-0927 (SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.
  25. APJ agonist

    CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias.
  26. androgen receptor modulator

    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  27. Smurf1 inhibitor

    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  28. glucocorticoid receptor modulator

    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
  29. GPR171 antagonist

    MS21570 is a selective GPR171 antagonist, with an IC50 of 220 nM.
  30. CB1 agonist

    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.
  31. 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.
  32. 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.
  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.
  34. 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.
  35. 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.
  36. 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.
  37. RORγt inverse agonist

    (Rac)-TMP778 is the racemate of TMP778. TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
  38. GPR35/CXCR8 agonist

    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  39. ACE inhibitor

    Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
  40. androgen receptor/CYP17A1 dual inhibitor

    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.

  41. Androgen receptor partial agonist

    YK11 is a partial agonist of androgen receptor, with osteogenic activity.
  42. Estrogen receptor antagonist

    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
  43. GPR40/FFAR1 agonist

    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  44. GPR84 antagonist

    GPR84 antagonist 8 is a selective GPR84 antagonist.
  45. 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.
  46. RORγt inverse agonist

    RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM.
  47. Azelaprag (Example 263.0) is an apelin receptor agonist drug candidate.
  48. Gpr120 agonist

    GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62.
  49. ROR gamma modulator

    Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
  50. Liothyronine sodium is a thyroid hormone (T3) analog. It promotes adipogenic differentiation of MSCs.

Items 351-400 of 1754

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