1. Immunology/Inflammation
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  3. Factor B-IN-8

Factor B-IN-8 (Compound (3R ,4R )-15) 是一种强效、选择性且具有口服活性的 B 因子 (factor B) 抑制剂,其 IC50 值为 10.2 nM。Factor B-IN-8 能有效抑制 B 因子与 C3b 的结合以及后续 C3 转化酶 (C3bBb) 的形成。Factor B-IN-8 可抑制旁路途径介导的膜攻击复合物 (MAC) 的沉积,其 IC50 值为 59.3 nM 。Factor B-IN-8 能够减少 B 因子蛋白的裂解,并降低补体 C3d 在肾小球和肾小管中的沉积。BFactor B-IN-8 可用于关节炎和阵发性睡眠性血红蛋白尿 (PNH) 的研究。

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Factor B-IN-8

Factor B-IN-8 Chemical Structure

CAS No. : 3049710-19-9

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  • 生物活性

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生物活性

Factor B-IN-8 (Compound (3R ,4R )-15) is a potent, selective and orally active factor B inhibitor with an IC50 of 10.2 nM. Factor B-IN-8 can effectively inhibit the binding of factor B to C3b and the subsequent formation of C3 convertase (C3bBb). Factor B-IN-8 can inhibit the deposition of membrane attack complex (MAC) mediated by alternativepathway with an IC50 of 59.3 nM. Factor B-IN-8 can reduce the cleavage of factor B protein and decrease the deposition of complement C3d in the glomeruli and renal tubules. Factor B-IN-8 can be used for researches of arthritis and paroxysmal nocturnal hemoglobinuria (PNH)[1].

药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Dog[1] 3 mg/kg i.v. T1/2 3.16 h
Dog[1] 6 mg/kg i.g. Tmax 0.46 h
Rat[1] 10 mg/kg i.v. T1/2 10.58 h
Rat[1] 20 mg/kg i.g. Tmax 0.38 h
Dog[1] 3 mg/kg i.v. Cmax 14947 ng/mL
Dog[1] 6 mg/kg i.g. T1/2 5.83 h
Rat[1] 10 mg/kg i.v. Cmax 16788 ng/mL
Rat[1] 20 mg/kg i.g. T1/2 9.28 h
Dog[1] 3 mg/kg i.v. AUC0-t 8333 ng·h/mL
Dog[1] 6 mg/kg i.g. Cmax 4680 ng/mL
Rat[1] 10 mg/kg i.v. AUC0-t 11413 ng·h/mL
Rat[1] 20 mg/kg i.g. Cmax 2659 ng/mL
Dog[1] 3 mg/kg i.v. AUC0-∞ 9487 ng·h/mL
Dog[1] 6 mg/kg i.g. AUC0-t 14388 ng·h/mL
Rat[1] 10 mg/kg i.v. AUC0-∞ 15313 ng·h/mL
Rat[1] 20 mg/kg i.g. AUC0-t 8793 ng·h/mL
Dog[1] 3 mg/kg i.v. Vss 1.23 L/kg
Dog[1] 6 mg/kg i.g. AUC0-∞ 16738 ng·h/mL
Rat[1] 10 mg/kg i.v. Vss 9.18 L/kg
Rat[1] 20 mg/kg i.g. AUC0-∞ 13505 ng·h/mL
Dog[1] 6 mg/kg i.g. F 86.77 %
Rat[1] 20 mg/kg i.g. F 51.82 %
分子量

462.46

Formula

C24H25F3N2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Factor B-IN-8
目录号:
HY-181040
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