Factor D inhibitor 7

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Factor D抑制剂7是一种有效的、选择性的、口服生物可利用的D因子抑制剂，IC50为50 nM。

Factor D inhibitor 7 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 50 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.

The highly specific S1 serine protease factor D (FD) plays a central role in the amplification of the complement alternative pathway (AP) of the innate immune system. Complement factor D-IN-1 (compound 2) shows similar potency against human and monkey FD (IC50s in FD thioesterolytic assays of 0.005 μM and in 50% serum MAC deposition assays of 0.011 μM for both human and monkey).

Complement factor D-IN-1 displays an excellent oral PK profile in Sprague–Dawley rats and, following an oral dose (10 mg/kg) in Brown Norway rats, demonstrates a good distribution and sustained exposure in ocular tissues including the neural retina and the posterior eye cup (PEC), which comprises the sclera, retinal pigmented epithelium, and choroid. Mean exposure levels in plasma, the PEC, and the retina at 6 h after dosing are 0.36, 0.43, and 0.09 μM, respectively.

FD inhibitor-2 | MDK55760 | MDK-55760 | MDK 55760 |

Immunology/Inflammation

Complement System

Complement System

Inflammation/Immunology

——

1386455-76-0

483.326

C21H19BrN6O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (517.26 mM)

O=C(C1=NN(CC(N2[C@]3([H])C[C@]3([H])C[C@H]2C(NC4=NC(Br)=CC=C4)=O)=O)C5=C1C=CC=C5)N

1-(2-((1R,3S,5R)-3-((6-bromopyridin-2-yl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1H-indazole-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years