货号	规格	价格	上海	北京	珠海	重庆	武汉
V47958-1mg	≥98%	￥1340.00 V47958-1mg ￥1340.00 3-5天	0 货期：3-5天	-	-	-	-
V47958-5mg	≥98%	￥2980.00 V47958-5mg ￥2980.00 3-5天	0 货期：3-5天	-	-	-	-
V47958-10mg	≥98%	￥4480.00 V47958-10mg ￥4480.00 3-5天	0 货期：3-5天	-	-	-	-
V47958-25mg	≥98%	￥8080.00 V47958-25mg ￥8080.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV 1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV 1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.

靶点：

HIV-1 (WT):0.081 μM (IC50)

体外研究：

HIV-1 inhibitor-8 (2 mg/kg; i.v.) shows a favorable mean CL, volume of distribution and a long terminal half-life.
HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours.

体内研究：

HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC50=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC50 value of 19.84 μM in CHO-hERG cells.

参考文献：

1. Wang Z, et al. Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01015.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.275 ml	11.376 ml	22.752 ml
5 mM	0.455 ml	2.275 ml	4.55 ml
10 mM	0.228 ml	1.138 ml	2.275 ml
50 mM	0.046 ml	0.228 ml	0.455 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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