Cathepsin C-IN-5|cas:2825567-97-1|西域试剂

Cathepsin C-IN-5,95.01%

产品编号：Bellancom-146584| CAS NO：2825567-97-1| 分子式：C₂₁H₁₇ClN₆OS| 分子量：436.92

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-146584	￥2500.00	杭州北京（现货）
Bellancom-146584	￥4000.00	杭州北京（现货）
Bellancom-146584	￥8500.00	杭州北京（现货）
Bellancom-146584	￥13500.00	杭州北京（现货）

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Cathepsin C-IN-5

产品介绍

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。

生物活性

Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC₅₀s 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.

体外研究

Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC₅₀s of 115.4, 70.2 nM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice.
Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07%.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 male mice (acute lung injury (ALI) mice model)
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 male mice (acute lung injury (ALI) mice model)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (45.77 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2887 mL	11.4437 mL	22.8875 mL
5 mM	0.4577 mL	2.2887 mL	4.5775 mL
10 mM	0.2289 mL	1.1444 mL	2.2887 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (4.58 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。