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Dexelvucitabine

Names

[ CAS No. ]:
134379-77-4

[ Name ]:
Dexelvucitabine

[Synonym ]:
Reverset
Dexelvucitabine
DFC
YZ-817
D-D4FC
2',3'-didehydro-2,3-dideoxy-5-fluorocytidine
INCB-8721
DPC-817

Biological Activity

[Description]:

Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful drug against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Reverse Transcriptase

[Target]

HIV-1


[In Vivo]

Dexelvucitabine (Reverset; d-d4FC; 33.3 mg/kg by i.v. or p.o.) has distribution and elimination half-lives (t1/2α and t1/2β, respectively) of 0.7 and 3.6 h in monkeys, respectively. The Cmax ranges from 21.1 to 47.5 μM[2]. Dexelvucitabine has a favorable pharmacokinetic profile with a long half-life (4.71 and 10.75 h after administration by the intravenous [i.v.] and oral [p.o.] routes, respectively) in woodchucks[2].

[References]

[1]. Brenda I Hernandez-Santiago, et al. Antiviral and cellular metabolism interactions between Dexelvucitabine and lamivudine. Antimicrob Agents Chemother. 2007 Jun;51(6):2130-5.

[2]. L Ma, et al. Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys. Antimicrob Agents Chemother. 1999 Feb;43(2):381-4.

Chemical & Physical Properties

[ Density]:
1.66g/cm3

[ Boiling Point ]:
394.9ºC at 760mmHg

[ Molecular Formula ]:
C9H10FN3O3

[ Molecular Weight ]:
227.19200

[ Flash Point ]:
192.6ºC

[ Exact Mass ]:
227.07100

[ PSA ]:
90.37000

[ Vapour Pressure ]:
7.15E-08mmHg at 25°C

[ Index of Refraction ]:
1.665

[ Storage condition ]:
2-8°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream