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C1s inhibitor (R)-8

Chemical Structure : C1s inhibitor (R)-8

CAS No.:

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C1s inhibitor (R)-8

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 422.44
Formula C22H20F2N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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