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[CAS NO. 134379-77-4] Dexelvucitabine
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14920 |
| Brand: | MCE |
| CAS: | 134379-77-4 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 227.19 |
| Molecular Formula | C9H10FN3O3 |
| SMILES | O=C1N(C=C(C(N)=N1)F)[C@]2([H])O[C@@H](C=C2)CO |
Summary
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] .
IC50 & 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 (t
1/2α
and t
1/2β
, respectively) of 0.7 and 3.6 h in monkeys, respectively. The C
max
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00300573 | Incyte Corporation |
HIV Infections|Human Immunodeficiency Virus
|
April 2006 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 220.08 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.4016 mL | 22.0080 mL | 44.0160 mL |
| 5 mM | 0.8803 mL | 4.4016 mL | 8.8032 mL |
| 10 mM | 0.4402 mL | 2.2008 mL | 4.4016 mL |
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.
Synonyms
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