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首页-小分子抑制剂&激动剂-GPCR-Relaxin Receptor -RXFP2 agonist 6641
RXFP2 agonist 6641

Chemical Structure : RXFP2 agonist 6641

CAS No.: 2971704-85-3

RXFP2 agonist 6641 (Compound 6641)

货号: PC-49427Not For Human Use, Lab Use Only.

RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).
    Compound 6641 is also activate the mouse RXFP2 receptor, does not activate either human or mouse RXFP1 receptors and RXFP3 or RXFP4 receptors.
    Compound 6641 is an allosteric agonist of RXFP2 that requires the RXFP2 transmembrane domain for activity.
    Compound 6641 (3-5 uM) induces gubernacular invagination in mouse embryos, induces osteoblast mineralization in human osteoblasts in vitro, specifically activates the mouse RXFP2 receptor in vivo.
    Compound 6641 treatment (10 mg/kg, PO) promotes bone formation in vivo.

    物理化学性质&存储条件

    分子量 787.377
    分子式 C29H19F9IN3O5
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-8-(3,5-bis(trifluoromethyl)phenyl)-2-(2-(2-iodo-4-(trifluoromethoxy)phenoxy)acetyl)-1,3,4,12a-tetrahydrobenzo[e]pyrazino[1,2-a][1,4]diazepine-6,12(2H,11H)-dione

    参考文献

    1. Esteban-Lopez M, et al. Commun Biol. 2022 Nov 4;5(1):1183.

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