[CAS NO. 160707-69-7] Apricitabine

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [160707-69-7]

Catalog

HY-14913

Brand

MCE

CAS

160707-69-7

DESCRIPTION [160707-69-7]

Overview

MDL	-
Molecular Weight	229.26
Molecular Formula	C8H11N3O3S
SMILES	O=C1N=C(N)C=CN1[C@@H]2S[C@H](CO)OC2

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

Summary

Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor ( K _i =0.08 μM), as well as inhibits DNA polymerases α, β, and γ with K _i value of 300 μM, 12 μM, and 112.25 μM, respectively ^[1] . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection ^[2].

IC50 & Target

HIV-1

In Vitro

Apricitabine (SPD754; AVX754) is against clinical isolates of HIV-1 in cultured PBMCs with IC ₅₀ values of 0.2 μM, 1.45 μM, 2.2 μM and 2.4 μM for HIV-1RF, Wild type, 3TC resistant, 3TC and AZT resistant, respectively ^[1] .
Apricitabine (SPD754; AVX754) has antiviral activities agsinst HIV-1 clinical isolates resistant to nucleoside reverse transcriptase inhibitors in MT-4 cells, exhibits Mean IC ₅₀ values of 20 μM, 25 μM, 30 μM,21 μM,55 μM,32 μM and 71 μM for HIV-1IIIB,Wild-type (control), Zidovudine-resistant, Lamivudine-resistant, Zidovudine-resistant/lamivudine-resistant, Abacavir-resistant and Stavudine-resistant viruses,respectively ^[2] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Apricitabine (SPD754; AVX754) (oral adminstation; 10 mg/kg; once a day) exhibits a good oral bioavailability of 68% for males and 69.4% for females rats. And the T _1/2 , AUC _0–∞ , T _max , C _max are 62.2 mins, 157.4 μg/min/ml and 37.3 mins, 1.16 μg/ml in female rats ^[1] .
Apricitabine (SPD754; AVX754) (intravenous injection; 10 mg/kg; once a day) exhibits the T _1/2 , AUC _0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats ^[1] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00352066	Avexa	HIV Infection	July 2006	Phase 1
NCT00334659	Avexa	HIV Infections	June 2006	Phase 1
NCT00612898	Avexa	HIV Infections	February 2008	Phase 2\|Phase 3
NCT00367952	Avexa	HIV Infection	August 2006	Phase 2
NCT00126880	Avexa	HIV Infections	July 2005	Phase 2
NCT00686270	Avexa	HIV Infections	May 2008	Phase 3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.