SID26681509; SID-26681509

生物活性靶点体外研究体内研究 SID26681509; SID-26681509 试剂级价格

CAS号:958772-66-2
英文名:SID 26681509
中文名:SID26681509; SID-26681509
CBNumber:CB82535696
分子式:C27H33N5O5S
分子量:539.65
MOL File:958772-66-2.mol

SID26681509; SID-26681509化学性质

熔点 :131 °C
密度 :1.298±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :<26.98mg/ml in DMSO; <5.4mg/ml in ethanol
形态 :solid
酸度系数(pKa) :8.75±0.43(Predicted)
颜色 :White

SID26681509; SID-26681509性质、用途与生产工艺

生物活性 SID 26681509 是一种有效的，可逆的，竞争性的，选择性的人组织蛋白酶 L (human cathepsin L) 抑制剂，IC50 为 56 nM。SID 2668150 抑制 Plasmodium falciparum 的体外繁殖，并抑制 Leishmania major，IC50 分别为 15.4 μM 和 12.5 μM。SID 26681509 对组织蛋白酶 G 没有抑制活性。
靶点

IC50: 56 nM (Human cathepsin L), 0.5 μM (Cathepsin V), 15.4 μM ( Plasmodium falciparum ), 12.5 μM ( Leishmania major )
体外研究

After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC ₅₀ of 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 ^-1 s ^-1 and koff = 2.2 × 10 ^-5 s ^-1 (K _i = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148.
SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC ₅₀ values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G.
SID 26681509 inhibits cathepsin V activity with an IC ₅₀ value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability.
体内研究

SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models.