SID26681509; SID-26681509
| 中文名称 | SID26681509; SID-26681509 |
|---|---|
| 中文同义词 | 化合物 T12909;化合物SID 26681509;SID 26681509,人组织蛋白酶L抑制剂 |
| 英文名称 | SID 26681509 |
| 英文同义词 | SID 26681509;S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate;N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide;SID26681509; SID-26681509;ML023;slow-binding,falciparu,Inhibitor,SID-26681509,propagation,Parasite,Leishmania,major,reversible,Cathepsin,inhibit,SID26681509,Plasmodium,malaria,SID 26681509,Thiocarbazate;L-Tryptophan, N-[(1,1-dimethylethoxy)carbonyl]-, 2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide |
| CAS号 | 958772-66-2 |
| 分子式 | C27H33N5O5S |
| 分子量 | 539.65 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 958772-66-2.mol |
| 结构式 |  |
SID26681509; SID-26681509 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，溶于 DMSO； <5.4mg/ml，在乙醇中 |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.75±0.43(Predicted) |
| 颜色 | 白色 |
IC50: 56 nM (Human cathepsin L), 0.5 μM (Cathepsin V), 15.4 μM ( Plasmodium falciparum ), 12.5 μM ( Leishmania major )
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.
SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-103353 | SID26681509; SID-26681509 SID 26681509 | 958772-66-2 | 1mg | 720元 |
| 2024/04/30 | HY-103353 | SID26681509; SID-26681509 SID 26681509 | 958772-66-2 | 5mg | 1800元 |