Complement factor D-IN-1

小分子

补体因子D-IN-1

Complement factor D-IN-1

C651435-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC 50 s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively. In Vitro 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 (IC 50 s in FD thioesterolytic assays of 0.005 μM and in 50% serum MAC deposition assays of 0.011 μM for both human and monkey). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 0.006 μM (FD), 0.05 μM (MAC)

补体因子 D-IN-1 是一种强效、选择性的小分子可逆因子 d 抑制剂，在 FD 硫酯酶荧光测定和 MAC 沉积测定中的 IC 50 s 分别为 0.006 和 0.05 μM。

1386455-76-0

C21H19BrN6O3

483.32 g/mol

86673884

C1[C@H]2[C@@H]1N([C@@H](C2)C(=O)NC3=NC(=CC=C3)Br)C(=O)CN4C5=CC=CC=C5C(=N4)C(=O)N

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

1S/C21H19BrN6O3/c22-16-6-3-7-17(24-16)25-21(31)15-9-11-8-14(11)28(15)18(29)10-27-13-5-2-1-4-12(13)19(26-27)20(23)30/h1-7,11,14-15H,8-10H2,(H2,23,30)(H,24,25,31)/t11-,14-,15+/m1/s1

CWZUTHDJLNZLCM-DFBGVHRSSA-N

C1C2C1N(C(C2)C(=O)NC3=NC(=CC=C3)Br)C(=O)CN4C5=CC=CC=C5C(=N4)C(=O)N

86673884

DMSO : 250 mg/mL (517.26 mM; Need ultrasonic)

2

5

5

482.07 Da

482.07 Da

123.000 Ų

31

0

753.000

0

1

2.200