Cathepsin C-IN-5|2825567-97-1|-陌孚医药/Medlife

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Cathepsin C-IN-5

目录号: PL15159 纯度: ≥95%

CAS No. :2825567-97-1

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中文名称	Cathepsin C-IN-5
英文名称	Cathepsin C-IN-5
英文别名	Acetamide, N-[3-[[5-chloro-2-[[5-(3-thienyl)-2-pyridinyl]amino]-4-pyrimidinyl]amino]phenyl]-;Cathepsin C-IN-5
Cas No.	2825567-97-1
分子式	C₂₁H₁₇ClN₆Os
分子量	436.92
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情	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 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.
性状	Solid
IC50 & Target[1][2]	IC50: 59.9 nM (Cat C); 4.26 μM (Cat L); >5 μM (Cat S); >5 μM (Cat B); >5 μM (Cat K)
体外研究(In Vitro)	Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC50s of 115.4, 70.2 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献	[1]. Chen X, et al. Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo. Eur J Med Chem. 2022 Jun 5;236:114368.

溶解度数据	In Vitro: DMSO : 20 mg/mL (45.77 mM; ultrasonic and warming and heat to 60°C)配制储备液

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