Temsavir

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Chemical Structure| 701213-36-7 同义名 : -
CAS号 : 701213-36-7
货号 : A128252
分子式 : C24H23N7O4
纯度 : 98%
分子量 : 473.48
MDL号 : MFCD22665723
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Temsavir demonstrates exceptional efficacy against a wide range of viral isolates, with EC50 values below 10 nM for the majority. It specifically shows an average EC50 of 0.7±0.4 nM against LAI virus, varying from 0.01 nM against the most susceptible virus to more than 2,000 nM against the least susceptible. Temsavir's cytotoxicity has been assessed across multiple cell types from different human tissues, revealing CC50 values greater than 200 μM in various cell lines, including MT-2, HEK293, HEp-2, HepG2, HeLa, HCT116, MCF-7, SK-N-MC, HOS, H292, and MDBK, after either 3 or 6 days of culture. However, lower CC50 values of 105 and 192 μM were noted in PM1 T cells and PBMCs, respectively, after 6 days, indicating low cytotoxicity in cell culture[1]. Moreover, Temsavir shows a broad antiviral activity spectrum against a panel of clinical isolates, with IC50 values ranging from subnanomolar levels to more than 0.1 µM, highlighting its broad-spectrum antiviral efficacy[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL

参考文献

[1]Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7), 3498-3507.

[2]Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11.