[CAS NO. 147127-20-6] Tenofovir

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PRODUCTS SPECIFICATIONS [147127-20-6]

Catalog

SLK-S1401

Brand

Selleck

CAS

147127-20-6

DESCRIPTION [147127-20-6]

Overview

MDL	MFCD00943794
Molecular Weight	287.21
Molecular Formula	C9H14N5O4P
SMILES	C([C@H](OCP(=O)(O)O)C)N1C=2C(N=C1)=C(N)N=CN2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.4818 mL	17.4089 mL	34.8177 mL
5 mM	0.6964 mL	3.4818 mL	6.9635 mL
10 mM	0.3482 mL	1.7409 mL	3.4818 mL
50 mM	-	-	-

Description

Tenofovir (GS-1278) blocks and hepatitis B virus infections.

Features

Tenofovir disoproxil fumarate is the prodrug form of tenofovir.

Targets

Reverse transcriptase ^[1]

In vitro

Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT.

In vivo

Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.

References

[1] Witvrouw M, et al. Antivir Ther, 2004, 9(1), 57-65.
[2] Miller MD, et al. Nucleosides Nucleotides Nucleic Acids, 2001, 20(4-7), 1025-1028.
[3] Ying C, et al. J Viral Hepat, 2000, 7(2), 161-165.
[4] Wainberg MA, et al. Antivir Ther, 1999, 4(2), 87-94.
[5] De Clercq E, et al. Clin Microbiol Rev, 2003, 16(4), 569-596.

Synonyms

Phosphonic acid, P-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-

Phosphonic acid, [[2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-, (R)-

Phosphonic acid, [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-

P-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic acid

(R)-9-(2-Phosphonomethoxypropyl)adenine

Tenofovir

PMPA

GS 1275

GS 1278

Tenefovir

[(2R)-1-(6-Aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid

([[(2R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)phosphonic acid