L-NIL
| 中文名称 | L-NIL |
|---|---|
| 中文同义词 | 化合物 T11805;N-(5-氨基-5-羧基戊)-乙脒;L-NIL,诱导型一氧化氮合成酶 (INOS) 的抑制剂 |
| 英文名称 | N-(5-AMINO-5-CARBOXYPENTYL)-ACETAMIDINE |
| 英文同义词 | N-(5-AMINO-5-CARBOXYPENTYL)-ACETAMIDINE;N-EPSILON-ACETIMIDOYL-L-LYSINE;N-EPSILON-ACETIMIDOYL-L-LYSIN-EPSILON;H-LYS(1-IMINOETHYL)-OH;H-LYS(ACETIMIDOYL)-OH;LYSINE(ACETIMIDOYL)-OH;N-(5-Amino-5-carboxypentyl;Ne-Acetimidoyl-L-lysine |
| CAS号 | 53774-63-3 |
| 分子式 | C8H17N3O2 |
| 分子量 | 187.24 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 53774-63-3.mol |
| 结构式 |  |
L-NIL 性质
| 沸点 | 335.2±52.0 °C(Predicted) |
|---|---|
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | -15°C |
| 溶解度 | 水：50 mg/ml（267.04mM）； DMSO：< 1 mg/mL（不溶或微溶） |
| 形态 | 固体 |
| 酸度系数(pKa) | 2.52±0.24(Predicted) |
| 颜色 | 白色至米白色 |
L-NIL 是诱导型一氧化氮合成酶 (iNOS) 的抑制剂，其对 miNOS 的 IC50 值为3.3 μM。
IC50: 3.3 μM (mouse inducible NO synthase), 92 μM (rat brain constitutive NO synthase)
L-NIL produces a concentration-dependent inhibition of both the mouse inducible NOS (miNOS) and the rat brain constitutive NOS (rcNOS) and is considerably more potent for miNOS. The IC 50 values for L-NIL with miNOS and rcNOS are 3.3 and 92 pM, respectively, indicating that L-NIL is 28-fold more selective for miNOS. In addition, L-NIL has approximately 6-fold greater potency for miNOS than either L-NMA or L-NNA.
L-NIL (10 and 30 mg/kg, IP) prevents the inflammation, oxidative stress and autophagy induced by renal IR in mice.
| Animal Model: | Adult male Balb/c (20-25 g). |
| Dosage: | 10 and 30 mg/kg. |
| Administration: | Intraperitoneally at the end of CLP and at 6 h after sepsis induction. |
| Result: |
Led to a negligible increase in plasma NGAL compared to sham mice.
Led to a significant decrease in both TLR4 and IL1βprotein contents and clusterin transcript. Showed an increase in NFAT5 mRNA levels, as compared with mice treated with vehicle. Promoted a decrease in AR protein expression, as compared with animals treated with vehicle. |