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 151-200 of 1456

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Catalog No.
Product Name
Application
Product Information
Citations
  1. progesterone receptor antagonist

    Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.
  2. 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.
  3. angiotensin receptor-neprilysin inhibitor

    LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure.
  4. estrogen receptor modulator

    Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM).
  5. Glucocorticoid receptor antagonist

    The antiglucocorticoid RU43044 exerted significant agonist activity and activated MMTV-Luc transcription in osteosarcoma cells but not human breast cancer cells.
  6. GPR119 agonist

    APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.
  7. androgen receptor modulator

    LGD-4033 is an investigational selective androgen receptor modulator for treatment of conditions such as muscle wasting and osteoporosis, currently under development by Ligand Pharmaceuticals.
  8. FFA4/GPR120 agonist

    GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
  9. Angiotensin I is formed by the action of renin on angiotensinogen.
  10. Angiotensin (1-7) is an endogenous peptide fragment that can be produced from Ang I or Ang II via endo- or carboxy-peptidases respectively.
  11. Angiotensin II (Ang II) is an octapeptide hormone that plays a central role in cardiovascular homeostasis.
  12. Angiotensin III is a hexapeptide formed as a result of a cleavage at the N-terminus of Angiotensin II, a key factor in the Renin-Angiotensin-Aldosterone (RAAS) system by angiotensinases located in red blood cells and the vascular beds of most tissues.
  13. Angiotensin 1/2 (1-9) is a peptide (ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS) containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.
  14. Acetyl Angiotensinogen (1-14),porcine, The protein encoded by the Angiotensinogen gene is known as pre-angiotensinogen or angiotensinogen precursor.
  15. Angiotensin 1/2 (1-5) is a peptide that contains the amino acids 1-5 and is converted from Angiotensin I/II.
  16. Angiotensin 1/2 (1-6) is a peptide that contains the amino acids 1-6 and is converted from Angiotensin I/II peptide.
  17. Angiotensin 1/2 + A (2 - 8), potent endogenous vasoconstrictor peptide; derivative of angiotensin (Ang) II.
  18. BNP (1-32), human is a brain natriuretic peptide secreted by the human heart in response to cardiac volume or pressure.
  19. Parathyroid hormone (PTH) is the most important endocrine regulator of calcium and phosphorus concentration in extracellular fluid, which is secreted by the chief cell of the parathyroid glands as a polypeptide containing 84 amino acids.
  20. Deoxycholic acid, extracted from Pig bile, Suitability:Ethanol,ether,three oxygen methane,acetone,acetic acid,alkali hydroxide and alkali carbonate solution.
  21. Estrogen modulator

    Bazedoxifene is a third generation selective modulator of estrogen receptor.
  22. ERRβ and ERRγ agonist

    DY131(GSK 9089) is a novel selective agonist of ERRα and ERRβ.
  23. GnRH agonist

    Leuprolide acetate is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors.
  24. Androgen receptor modulator

    MK-0773, one of selective androgen receptor modulators (SARMs), is a 4-aza-steroid that exhibited tissue selectivity in humans (IC50= 6.6 nM).
  25. progesterone receptor agonist

    Nestoron is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor.
  26. TRβ agonist

    Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM.
  27. ROR agonist

    SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ; increases transcription of RORα target genes; thought to increase p53 stability.
  28. RORα agonist

    SR3335 is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
  29. Progesterone receptor agonist

    Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.
  30. Estrogen receptor modulator

    Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  31. Renin inhibitor

    VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.
  32. Enkephalin-degrading and ACE inhibitor

    Spinorphin is an endogenous factor that exhibits inhibitory effects on enkephalin-degrading enzymes.
  33. GPR139 agonist

    JNJ 63533054 is a potent and selective GPR139 agonist with EC50 value of 16nm.
  34. AT1 receptor antagonist

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

  35. GPR119 agonist

    APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
  36. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  37. GPR84 agonist

    6-OAU is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
  38. LXRα inhibitor

    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
  39. 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).
  40. 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.
  41. 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)
  42. estrogen receptor downregulator and antagonist

    AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist.
  43. 17-Hydroxyprogesterone is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
  44. Estrogen receptor degrader

    Brilanestrant (GDC-0810, ARN-810??? is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.
  45. GnRH agonist

    Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity.
  46. SERD/SERM

    RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities.
  47. GnRH agonist

    Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.
  48. Versipelostatin is a novel GRP78/Bip molecular chaperone down-regulator of microbial origin that was isolated from the metabolite of Streptomyces versipellis strain 4083-SVS6.
  49. Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.
  50. PXR agonist

    SR-12813 is a pregnane X receptor (PXR) agonist.

Items 151-200 of 1456

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