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L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐用途

L-NIL dihydrochloride 是诱导型一氧化氮合成酶 (iNOS) 的抑制剂,其对 miNOS 的 IC50 值为3.3 μM。

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L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐名称

[ CAS 号 ]:
159190-45-1

[ 中文名 ]:
赖氨酸二氢氯化物

[ 英文名 ]:
L-NIL dihydrochloride

[英文别名 ]:

N(6)-acetimidoyl-L-lysine dihydrochloride
N-Ethanimidoyl-L-lysine dihydrochloride
l-n6-(1-iminoethyl)lysine dihydrochloride
L-Lysine, N-(1-iminoethyl)-, hydrochloride (1:2)

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐生物活性

[ 描述 ]:

L-NIL dihydrochloride 是诱导型一氧化氮合成酶 (iNOS) 的抑制剂,其对 miNOS 的 IC50 值为3.3 μM。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 一氧化氮合酶

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 3.3 μM (mouse inducible NO synthase), 92 μM (rat brain constitutive NO synthase)[3].

[体外研究]

L-NIL对小鼠诱导型一氧化氮合酶(miNOS)和大鼠脑组织型一氧化氮合酶(rcNOS)均有浓度依赖性抑制作用,对miNOS的抑制作用更大。带有miNOS和rcNOS的L-NIL的IC50值分别为3.3和92pm,表明L-NIL对miNOS的选择性高28倍。此外,L-NIL对miNOS的效力大约是L-NMA或L-NNA的6倍[2]。

[体内研究]

L-NIL(10和30 mg/kg,IP)可预防小鼠肾IR引起的炎症、氧化应激和自噬[1]。动物模型：成年雄性Balb/c(20-25g)[1]。剂量：10和30毫克/千克。给药：CLP结束时和脓毒症诱导后6小时腹腔注射。结果：与假小鼠相比,血浆NGAL的升高微不足道。导致TLR4和IL1ββ蛋白含量和clusterin转录物显著降低。与溶媒组相比,NFAT5 mRNA水平增加。与溶媒组相比,促进了AR蛋白表达的降低。

[参考文献]

[1]. Consuelo Pasten, et al. l-NIL prevents the ischemia and reperfusion injury involving TLR-4, GST, clusterin, and NFAT-5 in mice. Am J Physiol Renal Physiol. 2019 Apr 1;316(4):F624-F634.

[2]. Sharon Angela Tanuseputero, et al. Intravenous Arginine Administration Downregulates NLRP3 Inflammasome Activity and Attenuates Acute Kidney Injury in Mice with Polymicrobial Sepsis. Mediators Inflamm. 2020 May 11;2020:3201635.

[3]. W M Moore, et al. L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase. J Med Chem. 1994 Nov 11;37(23):3886-8.

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐物理化学性质

[ 沸点 ]:
369ºC at 760 mmHg

[ 分子式 ]:
C₈H₁₉Cl₂N₃O₂

[ 分子量 ]:
260.161

[ 闪点 ]:
177ºC

[ 精确质量 ]:
259.085419

[ PSA ]:
99.20000

[ LogP ]:
2.95030

[ 外观性状 ]:
固体

[ 储存条件 ]:
20°C

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐MSDS

详细MSDS(安全技术说明书)

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S37/39

[ 危险品运输编码 ]:
NONH for all modes of transport

L-n6-(1-亚氨基乙基)赖氨酸双盐酸盐文献

Effects of nitric oxide synthase deficiency on a disintegrin and metalloproteinase domain-containing protein 12 expression in mouse brain samples.

Mol. Med. Report. 12 , 2253-62, (2015)

A disintegrin and metalloproteinase domain-containing protein 12 (ADAM12) belongs to the ADAM family of transmembrane proteins. Via proteolysis, cell adhesion, cell-cell fusion, cell-matrix interactio...

Leptin administration activates irisin-induced myogenesis via nitric oxide-dependent mechanisms, but reduces its effect on subcutaneous fat browning in mice.

Int. J. Obes. 39(3) , 397-407, (2015)

BACKGROUND/OBJETIVES: Obese leptin-deficient ob/ob mice exhibit high adiposity and reduced muscle mass with leptin replacement promoting weight loss and inducing muscle accretion through PGC-1α-depend...

L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase.

J. Med. Chem. 37 , 3886, (1994)

L-N6-(1-Iminoethyl)lysine (L-NIL) has been synthesized and is shown to be both a potent and selective inhibitor of mouse inducible nitric oxide synthase (miNOS). L-NIL has an IC50 of 3.3 microM for mi...

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