2. Endocrinology

Endocrinology

Endocrinology

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Found in most species of the animal kingdom, the endocrine system consists of glands that secrete hormones, and receptors that detect and react to the hormones. In response to environmental stimuli, the endocrine system secretes hormones and uses them as chemical messengers to orchestrate physiological, developmental and reproductive changes that affect the entire body for a long period of time. In order to maintain the proper functioning of the body through its entire life cycle, the endocrine system utilizes a complex feedback mechanism to fine-tune the balance of hormones in the bloodstream. Even a slight disruption to endocrine system’s function can throw off the delicate balance of hormones in the human body and lead to an endocrine disorder, or endocrine disease, such as diabetes, adrenal insufficiency, hyper- or hypothyroidism, and polycystic ovary syndrome (PCOS).

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-182447
    Contragestazol 69095-83-6
    Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals.
    Contragestazol
  • HY-18252B
    (R)-Avanafil 1638497-26-3 98%
    (R)-Avanafil ((R)-TA1790) is a selective PDE5 inhibitor (IC50: 5.2 nM). (R)-Avanafil can be used for research of erectile dysfunction.
    (R)-Avanafil
  • HY-18252R
    Avanafil (Standard) 330784-47-9 98%
    Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil (Standard)
  • HY-182563
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide 72732-17-3
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition.
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide
  • HY-182689
    LY3358966 2187395-66-8 98%
    LY3358966 is an orally active sodium-dependent phosphate cotransporter 2b (NPT2b) inhibitor with a human IC50 of 32.4 nM, mouse IC50 of 43.9 nM, and rat of IC50 26.8 nM. LY3358966 inhibits NPT2b-mediated intestinal phosphate transport, decreases acute phosphate uptake into plasma, and increases fecal phosphate excretion. LY3358966 can be used for the research of renal disease.
    LY3358966
  • HY-182705
    Org 214444-0 914093-78-0
    Org 214444-0 is an orally active, nanomolar-potent and selective FSHR agonist, with EC50 values of 2.0 nM and 1.2 nM in human and rat (measured in CHO cells). Org 214444-0 activates human granulosa cells in vitro, supports rat follicular development and induces ovulation in vivo. Org 214444-0 can be used for the research of infertility.
    Org 214444-0
  • HY-182741
    RET-IN-32 2620629-32-3
    RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer.
    RET-IN-32
  • HY-182904
    GV-001 3082707-76-1
    GV-001 is a selective and orally active HDAC6 inhibitor with an IC50 of 1.18 nM against HDAC6. GV-001 selectively enhances α-tubulin acetylation, reduces sIL-6 and Collagen I levels, suppresses renal cyst growth, and upregulates PC1 expression. GV-001 can be used for the study of autosomal dominant polycystic kidney disease (ADPKD).
    GV-001
  • HY-183414
    C5aR antagonist-1 1257868-45-3
    C5aR antagonist-1 is a potent C5aR antagonist with an IC50 of < 5 nM. C5aR antagonist-1 is applicable to the research of crescentic and necrotizing glomerular lesions.
    C5aR antagonist-1
  • HY-18341F
    Biotin-(L-Thyroxine) 149734-00-9 98%
    Biotin-(L-Thyroxine) is the biotinylated L-Thyroxine (HY-18341). L-Thyroxine is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from Biotin-(L-Thyroxine) (T4).
    Biotin-(L-Thyroxine)
  • HY-18346S
    Mozavaptan-d6 2750534-83-7 98%
    Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
    Mozavaptan-d6
  • HY-183487
    M1R modulator-1 2257498-40-9
    M1R modulator-1 is an orally effective positive allosteric modulator of muscarinic M1R, with an IP value of 0.88 nM. M1R modulator-1 can be used in constipation-related research.
    M1R modulator-1
  • HY-183543
    URAT1/GLUT9-IN-2 3051509-32-8 98%
    URAT1/GLUT9-IN-2 is a selective, orally active URAT1/GLUT9 inhibitor, with an IC50 of 2.81 μM against URAT1 and an IC50 of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy.
    URAT1/GLUT9-IN-2
  • HY-183628
    MEAP 98%
    MEAP (2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine) is a NEDD9-STAT3 modulator. MEAP disrupts NEDD9-STAT3 interaction, driving STAT3 Y705 dephosphorylation. MEAP induces G2/M phase arrest. MEAP can be used for the research of anaplastic thyroid cancer.
    MEAP
  • HY-183636
    M353-0039 1185074-29-6
    M353-0039 is a selective UT-A2 inhibitor with a human IC50 of 0.35 μM. M353-0039 blocks urea transport mediated by UT-A2. M353-0039 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis.
    M353-0039
  • HY-183637
    E822-1968 1037259-63-4
    E822-1968 is an UT-A2 inhibitor with a human IC50 of 0.44 μM. E822-1968 blocks urea transport mediated by UT-A2. E822-1968 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis.
    E822-1968
  • HY-183684
    RET-IN-33 98%
    RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.
    RET-IN-33
  • HY-183729
    RET-IN-34 2222758-09-8 98%
    RET-IN-34 is a RET inhibitor with an IC50 of 0.89 nM. RET-IN-34 serves as a target protein ligand for PROTAC synthesis (Ligand for Target Protein for PROTAC). RET-IN-34 is applicable for the synthesis of PROTAC RET Degrader 2 (HY-183783). RET-IN-34 exhibits anticancer activity against medullary thyroid carcinoma. RET-IN-34 can be used in studies related to medullary thyroid carcinoma.
    RET-IN-34
  • HY-183783
    PROTAC RET Degrader 2
    PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.
    PROTAC RET Degrader 2
  • HY-183986
    SR210831C
    SR210831C is a highly selective, orally active retinoic acid receptor α (RARα) inhibitor with an IC50 of 0.051 nM. SR210831C suppresses spermatogenesis by reducing sperm count in house mice via acting on the early stages of spermatogenesis, and it does not cross the blood-testis barrier. SR210831C can be used in male contraception research.
    SR210831C
Cat. No. Product Name / Synonyms Application Reactivity