抑二肽素A
| 中文名称 | 抑二肽素A |
|---|---|
| 中文同义词 | 抑二肽素A ≥97%(-20℃) (HPLC);L-异亮氨酰-L-脯氨酰-L-异亮氨酸;三肽抑制剂IPI;脯氨抑素;抑二肽素A |
| 英文名称 | DIPROTIN A |
| 英文同义词 | n-(1-l-isoleucyl-l-prolyl)-l-isoleucin;n-(1-l-isoleucyl-l-prolyl)-l-isoleucine;DIPROTIN A H2O;DIPEPTIDYLPEPTIDASE IV INHIBITOR I;ILE-PRO-ILE;ILE-PRO-ILE H2O;H-ILE-PRO-ILE-OH;H-ILE-PRO-ILE-OH H2O |
| CAS号 | 90614-48-5 |
| 分子式 | C17H31N3O4 |
| 分子量 | 341.45 |
| EINECS号 | |
| 相关类别 | 酶底物;原料药;Chiral Reagents;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Pepetides;peptides |
| Mol文件 | 90614-48-5.mol |
| 结构式 |  |
抑二肽素A 性质
| 沸点 | 583.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.140±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | DMSO:250.0(最大浓度 mg/mL);732.17(最大浓度 mM) 水:67.08(最大浓度 mg/mL);196.44(最大浓度 mM) |
| 形态 | 白色至类白色固体。 |
| 酸度系数(pKa) | 3.72±0.22(Predicted) |
| 水溶解性 | Soluble in water at 1mg/ml |
| CAS 数据库 | 90614-48-5(CAS DataBase Reference) |
Diprotin A (Ile-Pro-Ile) 是二肽基肽酶 IV (DPP-IV) 的抑制剂。
IC50: DPP-IV
Diprotin A (100 μM; 30 minutes after CXCR4-blocker or Src-inhibitor treatment) induces the phosphorylation of Src [Tyr 416] and VE-cadherin [Tyr731] in hECs in both normoxia and H/R conditions in human endothelial cells and disrupts endothelial cell-to-cell junctions, which are attenuated by CXCR4 (receptor of SDF-1α)-blocker or Src-inhibitor.
Western Blot Analysis
| Cell Line: | Human endothelial cells [1] |
| Concentration: | 100 μM |
| Incubation Time: | 30 minutes after CXCR4-blocker or Src-inhibitor treatment |
| Result: | Induced the phosphorylation of Src [Tyr 416] and VE-cadherin [Tyr731] in hECs. |
Diprotin A (intraperitoneal injection; 70 μg/kg; twice daily; 7 days) increases the phosphorylation of Src and VE-cadherin and aggravates vascular leakage in the retinas. Collectively, Diprotin A induces vascular leakage by augmenting the SDF-1α/CXCR4/Src/VE-cadherin signaling pathway.
| Animal Model: | Streptozotocin-induced diabetic retinopathy model in wild-type C57/BL6 mice |
| Dosage: | 70 μg/kg |
| Administration: | Intraperitoneal injection; twice daily; 7 days |
| Result: | Induced vascular leakage by augmenting the SDF-1α/CXCR4/Src/VE-cadherin signaling pathway. |
安全信息
| WGK Germany | 3 |
|---|---|
| RTECS号 | NR4737000 |
| 提供商 | 语言 |
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英文
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