NCX 1000
目录号 : GC30334NCX1000是一种肝特异性NO供体,它来源于熊去氧胆酸。
Cas No.:401519-96-8
Sample solution is provided at 25 µL, 10mM.
NCX 1000 is a liver-specific NO donor compound derived from ursodeoxycholic acid (UDCA).
NCX-1000 (15 mg/kg, p.o.) prevents ascite formation, reduces collagen deposition in CCl4-treated rats. NCX-1000 administration almost completely reverts portal hypertension induced by CCl4, and reduces portal pressure in cirrhotic rats. NCX-1000 reverts HSC contraction induced by FCS, and also inhibits MCP-1 release from HSCs stimulated with TNF-α and IFN-γ[1]. NCX-1000 (28 mg/kg, p.o.) decreases portal pressure without affecting mean arterial pressure and heart rate in rats. NCX-1000 also reduces vasoconstriction by 60% caused by 30 μM NE in rats. Administration of NCX-1000 to BDL and sham operated rats results in a similar increase of nitrite/nitrate and cGMP concentrations in the liver[2].
[1]. Fiorucci S, et al. NCX-1000, a NO-releasing derivative of ursodeoxycholic acid, selectively delivers NO to the liver and protects against development of portal hypertension. Proc Natl Acad Sci U S A. 2001 Jul 17;98(15):8897-902. Epub 2001 Jul 10. [2]. Fiorucci S, et al. NCX-1000, a nitric oxide-releasing derivative of ursodeoxycholic acid, ameliorates portal hypertension and lowers norepinephrine-induced intrahepatic resistance in the isolated and perfused rat liver. J Hepatol. 2003 Dec;39(6):932-9.
Animal experiment: | Rats: On the first protocol, 54 rats, 12 animals/group unless specified, are randomly allocated to receive one of the following treatments: group 1 has phenobarbital induction and no further treatment; group 2 (16 animals) is treated with CCl4 twice a week for 8 weeks; group 3 has CCl4 twice a week plus UDCA (15 mg/kg); and group 4 has CCl4 twice a week plus NCX-1000 (15 mg/kg). NCX-1000 and UDCA are dissolved in carboxymethyl cellulose and administered daily by gavage. Animal weight is monitored daily through the study period, and the dosage of CCl4 is adjusted accordingly to the animal weight. At the end of the treatment surviving animals are killed by an overdose of uretane, and blood, ascitic fluid, and livers are collected. A portion of each liver is fixed in 10% formalin for histological evaluation. The remaining tissue is partitioned and immediately stored under frozen liquid nitrogen at -80°C until used. On the second protocol, 74 rats are randomly allocated to receive the same treatments as protocol 1. At the end of the study, surviving animals are tested for portal and arterial pressure measurement. |
References: [1]. Fiorucci S, et al. NCX-1000, a NO-releasing derivative of ursodeoxycholic acid, selectively delivers NO to the liver and protects against development of portal hypertension. Proc Natl Acad Sci U S A. 2001 Jul 17;98(15):8897-902. Epub 2001 Jul 10. |
Cas No. | 401519-96-8 | SDF | |
Canonical SMILES | CC1(C2([H])C(C)CCC(OC(C=CC(C=CC(OCCCCO[N+]([O-])=O)=O)=C3)=C3OC)=O)C(CC2)([H])C(C(CC4([H])CC(O)CC5)O)([H])C(C45C)([H])CC1 | ||
分子式 | C38H55NO10 | 分子量 | 685.84 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.4581 mL | 7.2903 mL | 14.5807 mL |
5 mM | 0.2916 mL | 1.4581 mL | 2.9161 mL |
10 mM | 0.1458 mL | 0.729 mL | 1.4581 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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