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L-NAME HCl 51298-62-5

Product Description

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L-NAME HCl

Molecular Weight: 269.69 L-NAME 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.


Biological Activity


NG-nitro-L-arginine methyl ester (L-NAME; at 0.1-100 mM) causes concentration-dependent inhibition of the Ca2(+)-dependent
endothelial NO synthase from porcine aortae. L-NAME causes an
endothelium-dependent contraction and an inhibition of the
endothelium-dependent relaxation induced by acetylcholine (ACh) in
aortic rings. In another research, Viability of rMC-1 cells or BREC in
25 mM glucose is significantly less than at 5 mM glucose, and this cell
death is inhibited by l-NAME in both cell types.


L-NAME (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in
mean systemic arterial blood pressure accompanied by bradycardia. L-NAME
(100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to
ACh and bradykinin. The increase in blood pressure and bradycardia
produced by L-NAME is reversed by L-arginine (30-100 mg kg-1, i.v.) in a
dose-dependent manner.


Protocol(Only for Reference)


Kinase Assay: [1]

Enzyme Assay The oxidation of L-arginine is monitored by the conversion of [3H]- or [14C]-arginine to L-citrulline which separates L-citrulline from L-arginine by Dowex 50x8-200 (Na) chromatography. Typical reaction mixtures (100 pL) contains 50 mM HEPES, pH 7.0, 8 pM tetrahydrobiopterin, 1 mM CaC12, 0.01 mg/mL calmodulin, 0.5 mM EDTA, 0.450 pM [14C]-arginine (30000 cpm), and 100-200 pM NADPH. The cNOS-catalyzed oxidation of NADPH to NADP+ is monitored by the reduction of absorbance at 340 nm with a Kontron 860 spectrophotometer in a volume of 300 pL. All reactions are at 30 ℃ unless otherwise indicated.


Cell Assay: [3]

Cell lines rMC-1 cells
Concentrations 1 mM
Incubation Time 5 days
Method rMC-1 cells are incubated in 5 or 25 mM glucose, with or without l-NAME (1 mM). Media is changed every other day for up to 5 days. BREC cells are incubated in 5 or 25 mM glucose as well as inhibitor as described above for 5 days. Cell death is determined by light microscopy using a hemocytometer and a 0.4% trypan blue dye exclusion method. The number of cells that do not exclude the dye is expressed per 1,000 total cells. A minimum of 800 cells is counted per assay (8 dishes, >100 cells counted per dish), and the assay is replicated three times on different days.





Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)






Chemical Information







Molecular Weight (MW) 269.69
Formula

C7H15N5O4.HCl

CAS No. 51298-62-5

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO <1 mg/mL (
Water 54 mg/mL (200.22 mM)
Ethanol <1 mg/mL (
In vivo Saline 30 mg/mL





Chemical Name L-Ornithine, N5-[imino(nitroamino)methyl]-, methyl ester, hydrochloride (1:1)










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