SID26681509; SID-26681509
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- CAS号:
- 958772-66-2
- 英文名:
- SID 26681509
- 英文别名:
- ML023;SID 26681509;SID26681509; SID-26681509;N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide;L-Tryptophan, N-[(1,1-dimethylethoxy)carbonyl]-, 2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide;S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate;slow-binding,falciparu,Inhibitor,SID-26681509,propagation,Parasite,Leishmania,major,reversible,Cathepsin,inhibit,SID26681509,Plasmodium,malaria,SID 26681509,Thiocarbazate
- 中文名:
- SID26681509; SID-26681509
- 中文别名:
- 化合物 T12909;化合物SID 26681509;SID 26681509,人组织蛋白酶L抑制剂
- CBNumber:
- CB82535696
- 分子式:
- C27H33N5O5S
- 分子量:
- 539.65
- MOL File:
- 958772-66-2.mol
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SID26681509; SID-26681509化学性质
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熔点:
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131 °C
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密度:
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1.298±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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<26.98mg/ml in DMSO; <5.4mg/ml in ethanol
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形态:
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solid
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酸度系数(pKa):
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8.75±0.43(Predicted)
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颜色:
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White
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SID26681509; SID-26681509性质、用途与生产工艺
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。
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.
SID26681509; SID-26681509
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
SID26681509; SID-26681509
生产厂家
958772-66-2, SID26681509; SID-26681509 相关搜索:
- 药靶配体
- SID 26681509,人组织蛋白酶L抑制剂
- 化合物SID 26681509
- 化合物 T12909
- 958772-66-2
- L-Tryptophan, N-[(1,1-dimethylethoxy)carbonyl]-, 2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide
- slow-binding,falciparu,Inhibitor,SID-26681509,propagation,Parasite,Leishmania,major,reversible,Cathepsin,inhibit,SID26681509,Plasmodium,malaria,SID 26681509,Thiocarbazate
- ML023
- SID26681509; SID-26681509
- N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide
- S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate
- SID 26681509