Home Immunology & Inflammation NOS 억제제 L-NAME HCl

연구용

L-NAME HCl NOS 억제제

제품 번호: S2877

L-NAME HCl(NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester)은 nNOS(소), eNOS(인간) 및 iNOS(쥐)에 대한 nitric oxide synthetases (NOS)의 비선택적 억제제이며, Ki 값은 각각 15 nM, 39 nM 및 4.4 μM입니다. 이 화합물은 고혈압 동물 모델을 유도하는 데 사용할 수 있습니다.
L-NAME HCl NOS 억제제 Chemical Structure

화학 구조

분자량: 269.69

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품질 관리 (Quality Control)

배치: 순도: 99.94%
99.94

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
mouse BV2 cells Function assay 24 h Inhibition of Nitric oxide synthase activity in mouse BV2 cells assessed as LPS-induced NO production after 24 hrs by Griess reaction, IC50=18.9 μM 21377368
mouse RAW264.7 cells Function assay 17-20 h Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-stimulated nitric oxide production after 17 to 20 hrs by Griess assay, IC50=27.13 μM 19359068
HUVEC Function assay Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by endothelial NOS (e NOS) from HUVEC cells, IC50=2.7μM 11327580
DLD-1 Function assay Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by inducible NOS (i NOS) from human DLD-1 cells, IC50=14μM 11327580
BV2 Function assay Inhibition of NOS-dependent nitric oxide production in mouse BV2 cells, IC50=36μM 17046255
BV2 Function assay Inhibition of nitric oxide synthase in mouse BV2 cells assessed as inhibition of LPS-induced NO production, IC50=20.1μM 18161942
BV2 Function assay Inhibition of iNOS-mediated NO production in LPS-induced mouse BV2 cells, IC50=25.8μM 18926710
BV2 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced iNOS-dependent nitrite production after 24 hrs by Griess method, IC50=25.8μM 21028898
BV2 Function assay Inhibition of iNOS in mouse BV2 microglial cells assessed as NO production, IC50=25.8μM 21115251
RAW264.7 Function assay 1 hr Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells preincubated with compound for 1 hr before exposure to LPS measured after 24 hrs by Griess reaction method, IC50=48.5μM 21435874
Sf9 Function assay 45 mins Inhibition of human recombinant eNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting, IC50=0.68μM 21923116
Sf9 Function assay 45 mins Inhibition of human recombinant nNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting, IC50=0.69μM 21923116
Sf9 Function assay 45 mins Inhibition of human recombinant iNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting, IC50=0.83μM 21923116
BV2 Function assay 24 hrs Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse BV2 cells measured after 24 hrs of post-stimulation by Griess reaction method, IC50=13.35μM 22115618
BV2 Function assay 1 hr Inhibition of LPS-induced NO production in mouse BV2 cells preincubated for 1 hr followed by LPS addition measured after 24 hrs by Griess assay, IC50=24.7μM 27588326
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation measured after 18 hrs by Griess assay, IC50=30.6μM 28099011
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RAW264.7 Anti-inflammatory assay 17 to 20 hr Anti-inflammatory activity in Mus musculus (mouse) RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-induced NO production after 17 to 20 hr by Griess assay, IC50=23.21μM ChEMBL
RAW264.7 Anti-inflammatory assay 17 to 20 hr Anti-inflammatory activity in Mus musculus (mouse) RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-induced nitric oxide production after 17 to 20 hr by Griess assay, IC50=26.21μM ChEMBL
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 269.69 화학식

C7H15N5O4.HCl

 보관 (수령일로부터)
CAS 번호 51298-62-5 SDF 다운로드 원액 보관

동의어 NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester Smiles COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl

용해도 (Solubility)

In vitro
배치:

Water : 54 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
nNOS
(Cell-free assay)
15 nM(Ki)
eNOS
(Cell-free assay)
39 nM(Ki)
시험관 내(In vitro)
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. This compound 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 this chemical in both cell types.
키나아제 분석
효소 분석
L-NAME HCl(Nω-nitro-L-arginine methyl ester hydrochloride)의 산화는 [3H]- 또는 [14C]-아르기닌이 L-시트룰린으로 전환되는 것을 모니터링하여 측정하며, 이는 Dowex 50x8-200 (Na) 크로마토그래피를 통해 L-시트룰린과 L-아르기닌을 분리합니다. 일반적인 반응 혼합물(100 pL)은 50 mM HEPES, pH 7.0, 8 pM 테트라하이드로바이오프테린, 1 mM CaC12, 0.01 mg/mL 칼모듈린, 0.5 mM EDTA, 0.450 pM [14C]-아르기닌(30000 cpm) 및 100-200 pM NADPH를 포함합니다. cNOS에 의한 NADPH에서 NADP+로의 산화는 Kontron 860 분광광도계를 사용하여 300 pL 부피에서 340 nm의 흡광도 감소를 통해 모니터링됩니다. 별도의 언급이 없는 한 모든 반응은 30 ℃에서 수행됩니다.
생체 내(In vivo)
L-NAME HCl (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. This compound (100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by this chemical is reversed by L-arginine (30-100 mg kg-1, i.v.) in a dose-dependent manner.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/9395704/

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(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2025-09-17)

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