产品名称

替诺福韦艾拉酚胺(Tenofovir Alafenamide)

一般描述

Tenofovir Alafenamide is a lipophilic phosphonamidate prodrug of tenofovir.

别 称

GS-7340

纯 度

≥99.0%(HPLC)

CAS NO.

379270-37-8

分子式

C²¹H²⁹N⁶O⁵P

分子量

476.474

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥25mg/mL

乙醇

≥25mg/mL

水

Insolube

l  生物学信息

生物活性/药理作用

Tenofovir Alafenamide is a lipophilic phosphonamidate prodrug of tenofovir, a synthetic antiviral acyclic nucleotide analog of adenosine 5-monophosphate and a nucleoside reverse tranase inhibitor (NRTI), with antiviral activity against hepatitis B virus (HBV) and potentially against human immunodeficiency virus (HIV). Upon oral administration, tenofovir alafenamide is taken up by hepatocytes through passive diffusion and through the hepatic uptake transporters organic anion transporting polypeptides 1B1 (OATP1B1) and 1B3 (OATP1B3). Inside the hepatocytes, tenofovir alafenamide is hydrolyzed and converted to tenofovir by carboxylesterase 1 (CES1). Intracellular tenofovir is phosphorylated by cellular kinases to its pharmacologically active form, tenofovir diphosphate. Tenofovir diphosphate is incorporated into viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate, and inhibits HBV reverse tranase, resulting in DNA chain termination and inhibition of HBV replication. In addition, tenofovir diphosphate is incorporated into HIV DNA  instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting HIV-1 reverse tranase (RT) and resulting in DNA chain termination and impairment of HIV replication.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.  https://www.ncbi.nlm.nih.gov