L-NAME hydrochloride is a nonselective inhibitor of nitric oxide synthetases (NOS) for nNOS (bovine), eNOS (human), and iNOS (murine), with Ki of 15 nM, 39 nM and 4.4 μM, respectively.
Oxid Med Cell Longev. 2021 Jun 14;2021:6662225.
Impaired Autophagy Induced by oxLDL/ β 2GPI/anti- β 2GPI Complex through PI3K/AKT/mTOR and eNOS Signaling Pathways Contributes to Endothelial Cell Dysfunction
L-NAME hydrochloride purchased from AbMole
|Source||Oxid Med Cell Longev (2021). Figure 5. (Abmole Bioscience, USA)|
|Method||Cell Culture and Treatment|
|Cell Lines||HUVECs and bEnd.3 cells|
|Incubation Time||4 h|
|Results||We found that LY294002, AZD5363, rapamycin, and L-NAME pretreatment could significantly upregulate the expression of LC3-II, while downregulating the expression of p62 compared with the oxLDL/β2GPI/anti-β2GPI complex alone group|
|Cell lines||H9C2 cells|
|Preparation method||H9C2 cells were exposed to hypoxia (2%O2; 4 h) or normoxic medium (21%O2; 4 h). After 4 h, culture medium was replaced with reoxygenated medium (21%O2 2 h) for H/R and normoxia controls, or hypoxic medium (2%O2; 2 h) in the presence and absence of 50 µM MnTBap or 100 µM L-NAME and then further incubated for 2 h in the presence of MTT reagent.|
|Incubation time||2 h|
|Animal models||Male Sprague-Dawley rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||Water: ≥ 30 mg/mL|
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Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.
Syzalterin is an inhibitor of NO production with an IC50 of 1.87 μg/mL.
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively.
L-NIL is an inducible NO synthase inhibitor, with an IC50 of 3.3 μM for miNOS.
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