CAThepsin C-IN-5 (compound SF38) 是一种有效的、选择性的和具有口服活性的组织蛋白酶 C抑制剂，CAT C、CAT L、CAT S、CAT B、CAT K 的IC50s 分别为 59.9 nM， 4.26 μM、>5 μM、>5 μM、>5 μM。CAThepsin C-IN-5 抑制骨髓和血液中的 CAT C 活性。CAThepsin C-IN-5 降低 NSP（中性粒细胞丝氨酸蛋白酶）的活化。CAThepsin C-IN-5 具有抗炎活性。

Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC 50 s of 59.9 nM, 4.26 μM, >5 μM, >5 μM, >5 μM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity [1].

Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC 50 s of 115.4, 70.2 nM, respectively [1].

Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice [1]. Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07% [1]. Cathepsin C-IN-5 (2, 10, 50 mg/kg; p.o.) shows effective antiinflammatory activity and potential protective effect in an animal model of ALI [1]. Animal Model: C57BL/6 male mice (acute lung injury (ALI) mice model) [1] Dosage: 2, 10, 50 mg/kg (one hour after administration, received LPS (20 mg/kg)) Administration: P.o. Result: Decreased the levels of proinflammatory cytokines (TNF-a, IL-6, and GM-CSF) and increased the the concentration of the anti-inflammatory cytokine (IL-10) in a dose-dependent manner.

C21H17ClN6OS

436.92

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years