53774-63-3
中文名稱
L-NIL
英文名稱
N-(5-AMINO-5-CARBOXYPENTYL)-ACETAMIDINE
CAS
53774-63-3
分子式
C8H17N3O2
分子量
187.24
MOL 文件
53774-63-3.mol
53774-63-3 結構式
基本信息
中文別名
N-(5-氨基-5-羧基戊)-乙脒 英文別名
H-LYS(ACETIMIDOYL)-OHH-LYS(1-IMINOETHYL)-OH
LYSINE(ACETIMIDOYL)-OH
Ne-Acetimidoyl-L-lysine
N-ε-Acetimidoyl-L-lysine
N-(5-Amino-5-carboxypentyl
L-Lysine, N6-(1-iMinoethyl)-
N-EPSILON-ACETIMIDOYL-L-LYSINE
N-EPSILON-ACETIMIDOYL-L-LYSIN-EPSILON
N-(5-AMINO-5-CARBOXYPENTYL)-ACETAMIDINE
物理化學性質
沸點335.2±52.0 °C(Predicted)
密度1.22±0.1 g/cm3(Predicted)
儲存條件-15°C
溶解度Water: 50 mg/mL (267.04 mM); DMSO: < 1 mg/mL (insoluble or slightly soluble)
酸度系數(pKa)2.52±0.24(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
L-NIL 是誘導型一氧化氮合成酶 (iNOS) 的抑制劑，其對 miNOS 的 IC50 值為3.3 μM。靶點
IC50: 3.3 μM (mouse inducible NO synthase), 92 μM (rat brain constitutive NO synthase)
體外研究
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.
體內研究
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 IL1β?protein 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. |