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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Complement System-C1s inhibitor (R)-8
C1s inhibitor (R)-8

Chemical Structure : C1s inhibitor (R)-8

CAS No.:

C1s inhibitor (R)-8

货号: PC-20646Not For Human Use, Lab Use Only.

C1s inhibitor (R)-8 is a potent, selective, orally available, and brain-penetrable C1s inhibitor with IC50 of 36 nM, effectively blocks the classical complement pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

C1s inhibitor (R)-8 is a potent, selective, orally available, and brain-penetrable C1s inhibitor with IC50 of 36 nM, effectively blocks the classical complement pathway.
(R)-8 shows excellent selectivity over C1r, MASP2, factor D, thrombin, trypsin, kallikrein, and plasmin (IC50>30 uM).
(R)-8 effectively inhibits membrane attack complex (MAC) formation in the in vitro assay system.
(R)-8 is orally available and brain-penetrable in mice.
(R)-8 is a valuable tool compound for both in vitro and in vivo assessment.

物理化学性质&存储条件

分子量 422.44
分子式 C22H20F2N6O
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

NC1=NN=CC2=C1C(F)=CC(N3C[C@H](C4=NOC(C)=C4)N(C5=CC=CC(F)=C5)CC3)=C2

参考文献

1. Zenichi Ikeda, et al. J. Med. Chem. 2023

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