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
Product Citation
  1. ERbeta agonist

    Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.
  2. Aromatase inhibitor

    Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
  3. Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells.
  4. nuclear estrogen receptor modulator

    Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator.
  5. dissociated glucocorticoid receptor agonist

    Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
  6. glucocorticoid receptor agonist

    Dagrocorat (PF-00251802) is a novel and dissociated glucocorticoid receptor agonist.
  7. ER β ligand

    DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β(ER β) selective ligand.
  8. Betamethasone (hydrochloride) is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.
  9. DP1 antagonist

    L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
  10. estrogen receptor degrader

    GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
  11. glucocorticoid receptor agonist

    (S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
  12. testosterone 5-alpha-reductase inhibitor

    Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor.
  13. 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.
  14. Angiotensin-II subtype 2 receptor(AT2 R) agonist

    CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
  15. angiotensin II receptor antagonist

    Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist.
  16. 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.
  17. PGD2) receptor type 2 (DP2) antagonist

    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
  18. estrogen receptor modulators

    Pipendoxifene hydrochloride is a selective estrogen receptor modulators (SERMs).
  19. estrogen receptor covalent antagonist

    H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).
  20. SARD ligand

    (R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
  21. 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).
  22. thyroid hormone receptor agonist

    Eprotirome is a liver-selective thyroid hormone receptor agonist.
  23. (±)-Equol is the racemate of equol. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
  24. progesterone receptor agonist

    Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.
  25. oestrogen receptor antagonist

    Enclomiphene citrate is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property.
  26. 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.
  27. direct renin inhibitor

    Aliskiren D6 Hydrochloride (CGP 60536 D6 Hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor with IC50 of 1.5 nM.
  28. glucocorticoid receptor agonist

    Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
  29. GPR55 antagonist

    ML191 (CCG-152883, CID-23612552) is an antagonist of GPR55 with EC50 of 1.076 ?M in U2OS cells overexpressing GPR55.
  30. estrogen receptor (ER) inhibitor

    WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity.
  31. antiestrogenic properties

    FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
  32. selective androgen receptor modulator

    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM.
  33. androgen receptor modulator

    AC-262536 is a selective androgen receptor (SAR) molecule. It has partial agonist activity with respect to testosterone and suppresses luteinizing hormone.
  34. ERRα agonist

    Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  35. modulator of estrogen receptor ER-alpha36

    SNG-1153 is a modulator of estrogen receptor ER-alpha36.
  36. 5α-reductase inhibitor

    Finasteride Carboxaldehyde is a metabolite of Finasteride in human bile (M2 metabolite) that can be used for proteomics research.
  37. Antiandrogenic agent

    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities.
  38. synthetic glucocorticoid receptor agonist

    Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation.
  39. GPR109A agonist

    Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
  40. Estrogen receptor degrader

    SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD).
  41. Androgen receptor antagonist

    TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist.
  42. RORγt inverse agonist

    TMP778 is a novel, potent, and selective RORγt inverse agonist.

  43. 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.
  44. GnRH peptide agonist

    Triptorelin is a synthetic gonadotropin-releasing hormone (GnRH) peptide agonist that binds to the GnRH receptor. It inhibits the growth of DU145, LNCaP, and PC3 prostate and OVCAR-3 ovarian cancer cells.
  45. GnRH receptor antagonist

    Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  46. prostanoid agonist

    QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.
  47. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation.
  48. ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways.
  49. (Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS.
  50. LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer.

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