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首页-小分子抑制剂&激动剂-GPCR-CGRP Receptor-FE 205030
FE 205030

Chemical Structure : FE 205030

CAS No.:

FE 205030 (FE205030)

货号: PC-72787Not For Human Use, Lab Use Only.

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.

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

    生物&药学活性

    FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.
    FE 205030 displays>100,000 fold against hAM1R and >6363 fold against hAM2R tested in Human CGRP, AM1R and AM2R receptor cAMP assays.
    FE 205030 inhibited CGRP-induced vasodilation in isolated human mesenteric resistance arteries in an ex vivo isometric myograph study; effectively blocked CGRP-induced vasodilation with a pA2 of 9.3.
    FE 205030 is a first in class injectable fast acting selective and potent agent for the treatment of acute episodic migraine.

    物理化学性质&存储条件

    分子量 1397.59
    分子式 C64H84N16O16S2
    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

    Oxazole-2-carbonyl-D-Val-Phe(2-Cbm)-c(Cys-Orn(iPr)-Asp-Val-Gly-Pro-Phe-Cys)-3Pal- NH2

    参考文献

    1. Karthik Srinivasan, et al. J Pharm Sci. 2022 Jan;111(1):247-261.

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