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。
| Cas No. | 2825567-97-1 |
| 分子式 | C21H17ClN6OS |
| 分子量 | 436.92 |
| 储存条件 | 4°C, away from moisture and light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally activeCathepsin Cinhibitor withIC50s 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 IC50s 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. |
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