性能参数

产品名称

Raltegravir potassium salt

规格

5mg 10mg 50mg 100mg

货号

GOY-Y3245

 含量

>98.00%

CAS

871038-72-1

别名

化学名

potassium (Z)-4-(((4-fluorobenzyl)imino)(hydroxy)methyl)-1-methyl-2-(2-(5-methyl-1,3,4-oxadiazole-2-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidin-5-olate

分子式

C20H20FKN6O5

分子量

分子量 482.51

溶解度

DMF: 1 mg/ml,DMSO: 2 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Raltegravir (potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.

PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme[1]. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity[2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium[3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication[4]. In acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range[5].

Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy[5].

四丁基硼氢化铵  33725-74-5  4-甲氧基-2-硝基苯甲酸  33844-21-2

2,3-吡啶二甲酸  339155-13-4  1-辛烯-3-醇  3391-86-4

2,6-二甲氧基苯甲醛  3392-97-0  3,5-二甲基-4-溴吡唑  3398-16-1

(2R,4S)-4-羟基吡咯烷-2-羧酸  3398-22-9  4-氯甲基苯甲酸甲酯  34040-64-7

3-氯-4-甲基苯甲醛  551949  L-酪氨酸甲酯盐酸盐  3417-91-2

6-甲基吲哚  555208  ?

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