1919853-46-5
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- CAS号:
- 1919853-46-5
- 英文名:
- PTP1B-IN-2
- 英文别名:
- MDK3465;PTP1B-IN-2;PTP1B inhibitor 2;PTP1B-IN-2;PTP1B INHIBITOR 2;Inhibitor,PTP-1B-IN-2,inhibit,PTP1BIN2,Phosphatase,PTP1B IN 2;Benzoic acid, 5-[[[4-[(2-methoxy-2-oxoethyl)(methylsulfonyl)amino]phenyl]methyl][(phenylmethyl)sulfonyl]amino]-2-[(4-methylphenyl)methoxy]-, methyl ester
- 中文名:
- 1919853-46-5
- 中文别名:
- 化合物PTP1B-IN-2;5-(N-(4-(N-(2-甲氧基-2-氧代乙基)甲基磺酰氨基)苄基)-1-苯基甲基磺酰氨基)-2-((4-甲基苄基)氧基)苯甲酸甲酯
- CBNumber:
- CB03309540
- 分子式:
- C34H36N2O9S2
- 分子量:
- 680.79
- MOL File:
- 1919853-46-5.mol
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1919853-46-5化学性质
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沸点:
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813.4±75.0 °C(Predicted)
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密度:
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1.350±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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DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: insol; PBS (pH 7.2): insol
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形态:
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A solid
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酸度系数(pKa):
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-3.81±0.50(Predicted)
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1919853-46-5性质、用途与生产工艺
PTP1B-IN-2 (MDK3465, Ptp1B-In-2, Compound P6)是一种有效的、选择性的 protein tyrosine phosphatase-1B (PTP1B) 抑制剂，其IC50值为50 nM。PTP1B-IN-2 可增强胰岛素介导的胰岛素受体β(IRβ)磷酸化，以及胰岛素刺激的葡萄糖的摄取。
| Target | Value |
PTP1B
(Cell-free assay)
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50 nM
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PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 µM and 30 µM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 µM, respectively .
1919853-46-5
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-100462 | 1919853-46-5
PTP1B-IN-2 | 1919853-46-5 | 1mg | 681元 |
| 2024/01/25 | HY-100462 | 1919853-46-5
PTP1B-IN-2 | 1919853-46-5 | 5mg | 1200元 |
1919853-46-5, 1919853-46-5 相关搜索:
- 药靶配体
- 化合物PTP1B-IN-2
- 5-(N-(4-(N-(2-甲氧基-2-氧代乙基)甲基磺酰氨基)苄基)-1-苯基甲基磺酰氨基)-2-((4-甲基苄基)氧基)苯甲酸甲酯
- 1919853-46-5
- Benzoic acid, 5-[[[4-[(2-methoxy-2-oxoethyl)(methylsulfonyl)amino]phenyl]methyl][(phenylmethyl)sulfonyl]amino]-2-[(4-methylphenyl)methoxy]-, methyl ester
- Inhibitor,PTP-1B-IN-2,inhibit,PTP1BIN2,Phosphatase,PTP1B IN 2
- PTP1B-IN-2;PTP1B INHIBITOR 2
- PTP1B inhibitor 2
- MDK3465
- PTP1B-IN-2