[CAS NO. 134379-77-4] Dexelvucitabine

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PRODUCTS SPECIFICATIONS [134379-77-4]

Catalog

HY-14920

Brand

MCE

CAS

134379-77-4

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : 50 mg/mL ( 220.08 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Cytidine, 2′,3′-didehydro-2′,3′-dideoxy-5-fluoro-

2′,3′-Didehydro-2′,3′-dideoxy-5-fluorocytidine

RA 131423

D-d 4FC

Reverset

DOC 817

INCB 8721

Dexelvucitabine

DPC 817

YZ 817

DFC

4-Amino-5-fluoro-1-[5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-1,2-dihydropyrimidin-2-one