L-NAME HCl

別名: NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester

目錄號(hào)：S2877 Purity: 99.94%

L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester)是一種無(wú)選擇性的一氧化氮合成酶抑制劑，對(duì)nNOS (牛源), eNOS (人源)和iNOS (鼠源)的K_i值分別為15nM, 39 nM和4.4 μM。L-NAME HCl 可用于誘導(dǎo)高血壓動(dòng)物模型。

L-NAME HCl Chemical Structure

CAS: 51298-62-5

規(guī)格	價(jià)格	庫(kù)存
100mg	647.01	現(xiàn)貨
1g	3030.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.94%

99.94

L-NAME HCl相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	nNOS eNOS iNOS	點(diǎn)擊展開
相關(guān)產(chǎn)品	1400W 2HCl Falcarindiol L-NMMA acetate TPEN 2',5'-Dihydroxyacetophenone	點(diǎn)擊展開
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 高選擇性抑制劑庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
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
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
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
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
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	Function assay		Inhibition of iNOS in mouse BV2 microglial cells assessed as NO production, IC50=25.8μM	21115251
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

nNOS ^[1] (Cell-free assay)	eNOS ^[1] (Cell-free assay)
15 nM(Ki)	39 nM(Ki)

體外研究(In Vitro)
體外研究活性	NG-硝基-L-精氨酸甲酯(L-NAME; 0.1-100 mM)濃度依賴性抑制豬主動(dòng)脈中Ca₂(+)-依賴性內(nèi)皮NO合酶。L-NAME引起主動(dòng)脈環(huán)中內(nèi)皮細(xì)胞依賴性收縮，以及乙酰膽堿(ACh)誘導(dǎo)的血管內(nèi)皮依賴性舒張反應(yīng)的抑制。^[2]在另一項(xiàng)研究中，rMC-1細(xì)胞或BREC在25 mM葡萄糖中的活性顯著比在5 mM葡萄糖中低，這種細(xì)胞死亡在兩種細(xì)胞類型中被l-NAME抑制。^[3]
激酶實(shí)驗(yàn)	酶測(cè)定
激酶實(shí)驗(yàn)	L-精氨酸的氧化通過[³H]-或[¹⁴C]-精氨酸轉(zhuǎn)化為L(zhǎng)-瓜氨酸監(jiān)測(cè)，通過Dowex 50x8-200 (Na)色譜分析從L-精氨酸中分離L-瓜氨酸。典型的反應(yīng)混合物(100 pL)包含50 mM HEPES，pH 7.0，8 pM 四氫生物蝶呤，1 mM CaC1₂，0.01 mg/mL鈣調(diào)蛋白，0.5 mM EDTA，0.450 pM [¹⁴C]-精氨酸(30000 cpm)，和100-200 pM NADPH。NADPH被cNOS催化氧化為NADP+，通過Kontron 860分光光度計(jì)，在300 pL體積中340 nm下吸光度的減少監(jiān)測(cè)。除非另有說明，所有反應(yīng)在30 ℃下進(jìn)行。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	rMC-1細(xì)胞
	濃度	1 mM
	孵育時(shí)間	5天
	方法	rMC-1細(xì)胞與5或25mM葡萄糖，l-NAME (1 mM)存在或不存在下培育。培養(yǎng)基每隔一天更換，進(jìn)行5天。BREC細(xì)胞與5或25mM葡萄糖以及抑制劑在上述條件下培育5天。細(xì)胞死亡通過光學(xué)顯微鏡使用血細(xì)胞計(jì)數(shù)器和0.4%臺(tái)盼藍(lán)染色排除法測(cè)定。沒有被染料排除的細(xì)胞數(shù)量以每1,000個(gè)總細(xì)胞表達(dá)。每個(gè)試驗(yàn)至少計(jì)數(shù)800個(gè)細(xì)胞(8個(gè)培養(yǎng)皿，每個(gè)培養(yǎng)皿細(xì)胞計(jì)數(shù)>100)，并且試驗(yàn)在不同的日子重復(fù)三次。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	L-NAME(0.03-300 mg kg-1, i.v.)誘導(dǎo)平均全身動(dòng)脈血壓劑量依賴性增加，伴隨心動(dòng)過緩。L-NAME (100 mg kg-1, i.v.)顯著抑制對(duì)Ach和緩激肽的降壓反應(yīng)。L-NAME引起的血壓增加和心動(dòng)過緩被L-arginine (30-100 mg kg-1, i.v.)劑量依賴性逆轉(zhuǎn)。^[2]
動(dòng)物實(shí)驗(yàn)	Animal Models	雄性Wistar大鼠
	Dosages	100 mg/kg
	Administration	i.v.

參考文獻(xiàn)
[1] Furfine ES, et al. Biochemistry, 1993, 32(33), 8512-8517. [2] Rees DD, et al. Br J Pharmacol, 1990, 101(3), 746-752. [3] Du Y, et al. J Physiol Regul Integr Comp Physiol, 2004, 287(4), R735-R741. [4] Heggers JP, et al. J Altern Complement Med, 1997, 3(2), 149-153. + 展開

參考文獻(xiàn)

[1] Furfine ES, et al. Biochemistry, 1993, 32(33), 8512-8517.
[2] Rees DD, et al. Br J Pharmacol, 1990, 101(3), 746-752.
[3] Du Y, et al. J Physiol Regul Integr Comp Physiol, 2004, 287(4), R735-R741.

[4] Heggers JP, et al. J Altern Complement Med, 1997, 3(2), 149-153.

+ 展開