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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Integrin-GSK3008348
GSK3008348

Chemical Structure : GSK3008348

CAS No.: 1629249-33-7

GSK3008348 (GSK-3008348)

货号: PC-60069Not For Human Use, Lab Use Only.

GSK3008348 is a potent, selective, RGD-mimetic integrin αvβ6 antagonist with KD value of 9.5 pM and 4.8 pM for αvβ6 in normal and IPF human lung tissue membrane preparations.

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

生物&药学活性

GSK3008348 is a potent, selective, RGD-mimetic integrin αvβ6 antagonist with KD value of 9.5 pM and 4.8 pM for αvβ6 in normal and IPF human lung tissue membrane preparations.
GSK3008348 exhibits a high affinity and a minimum of 26-fold selectivity for the αvβ6 integrin over the other RGD integrin family members.
GSK3008348 induces αvβ6 internalization and degradation in human lung epithelial cells.
GSK3008348 engages αvβ6, induces prolonged inhibition of TGFβ signaling and reduces lung collagen deposition and serum C3M, a marker of IPF disease progression, in murine bleomycin-induced lung fibrosis model.

物理化学性质&存储条件

分子量 487.636
分子式 C29H37N5O2
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

(3S)-3-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-4-{(3S)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinyl}butanoic acid

参考文献

1. John AE, et al. Nat Commun. 2020 Sep 16;11(1):4659.

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