Danoprevir (RG7227)

产品编号: DC8238 Featured
Danoprevir (RG7227)
结构式
850876-88-9
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中国地区超过5000个高品质化合物库存
应用领域
Danoprevir (ITMN-191) 是一种具有口服活性的 NS3/4A蛋白酶抑制剂,IC50 值为 0.29 nM。与其他 53 种蛋白酶 (IC50高于 10 μM) 相比,对 NS3/4A 具有高选择性。Danoprevir (ITMN-191) 抑制 HCV 基因型 1a, 1b, 4, 5, 6 (IC50s=0.2-0.4 nM) 和 2b, 3a (IC50s=1.6, 3.5 nM)。
Cas No.: 850876-88-9
名称: dimethylethoxy)carbonyl]amino]-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydro-5,16-dioxocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-2-yl ester Danoprevir (ITMN-191)
别名: ITMN-191; R7227; RO5190591; RG7227,ITMN191,ITMN 191
SMILES: CC(C)(C)OC(=O)N[C@H]1CCCCC/C=C/[C@@H]2C[C@]2(NC(=O)[C@@H]3C[C@H](CN3C1=O)OC(=O)N4CC5=C(C4)C(=CC=C5)F)C(=O)NS(=O)(=O)C6CC6
分子式: C35H46FN5O9S
分子量: 731.83
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Danoprevir is an inhibitor of the NS3/4A protease.Danoprevir (ITMN 191; ITMN-191; R7227; RO5190591; RG7227)is useful for anti-HCV,anti-cancer. Danoprevir (0.29 nM) inhibits the reference genotype 1 NS3/4A protease half-maximally, but a high dose of Danoprevir (10 μM) shows no appreciably inhibition in a panel of 79 proteases, ion channels, transporters, and cell surface receptors. Danoprevir remains bound to and inhibits NS3/4A for more than 5 hours after its initial association. Danoprevir (45 nM) eliminates a patient-derived HCV genotype 1b replicon from hepatocyte-derived Huh7 cells with an EC50 of 1.8 nM. In HCV subgenomic replicon cell lines containing the individual mutations, V36M, R109K, and V170A substitutions confer little or no resistance to Danoprevir, but the R155K substitution confers a high level (62-fold increase) of resistance to Danoprevir. In Huh7.5 cells transfected with chimeric recombinant virus, Danoprevir shows antiviral inhibition effects against HCV genotypes 1, 4 and 6 with IC50 of 2-3 nM, which are >100-fold lower than genotypes 2/3/5 (280-750 nM). For the detailed information of Danoprevir (RG7227), the solubility of Danoprevir (RG7227) in water, the solubility of Danoprevir (RG7227) in DMSO, the solubility of Danoprevir (RG7227) in PBS buffer, the animal experiment (test) of Danoprevir (RG7227), the cell expriment (test) of Danoprevir (RG7227), the in vivo, in vitro and clinical trial test of Danoprevir (RG7227), the EC50, IC50,and affinity,of Danoprevir (RG7227), For the detailed information of Danoprevir (RG7227), the solubility of Danoprevir (RG7227) in water, the solubility of Danoprevir (RG7227) in DMSO, the solubility of Danoprevir (RG7227) in PBS buffer, the animal experiment (test) of Danoprevir (RG7227), the cell expriment (test) of Danoprevir (RG7227), the in vivo, in vitro and clinical trial test of Danoprevir (RG7227), the EC50, IC50,and affinity,of Danoprevir (RG7227), Please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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