SID 26681509 是可逆的,竞争性的人组织蛋白酶 L选择性抑制剂,IC50为 56 nM。它抑制PlaSmodium falciparum的体外繁殖,IC50为15.4 μM,抑制Leishmania major,IC5012.5 μM。
产品描述
SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).
体外活性
After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent(IC50 : 1.0 nM). SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148[1]. SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values determined after one hour ranging from 618 nM to 8.442 μM[1].
体内活性
survival in murine models of sepsis significantly improved SID 26681509 by and reduces liver damage following warm liver ischemia/reperfusion (I/R) models[2].
Cas No.
958772-66-2
分子式
C27H33N5O5S
分子量
539.65
储存和溶解度
DMSO:55 mg/ml (101.92 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years