- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 160707-69-7] Apricitabine
| 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-14913 |
| Brand: | MCE |
| CAS: | 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 |
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.
Apricitabine Related Antibodies
- CDT1 Antibody
- Hes1 Antibody
- JunB Antibody
- Nanog Antibody
- PCNA Antibody
- S100A4 Antibody
- SP1 Antibody
- BRCA1 Antibody (YA819)
- Elongation Factor 1A1 Antibody
- KAP1 Antibody
- MCM2 Antibody (YA705)
- MLH1 Antibody (YA703)
- RNA Polymerase II Subunit B1 Antibody
- RPA70 Antibody (YA678)
- MCM2 Antibody
- MLH1 Antibody
- PDX1 Antibody
- RbAP48 Antibody
- RbBP5 Antibody
- Argonaute 2 Antibody (YA612)
- S100A6 Antibody (YA674)
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.
References
- [1] de Muys JM, et al. Anti-human immunodeficiency virus type 1 activity, intracellular metabolism, and pharmacokinetic evaluation of 2'-deoxy-3'-oxa-4'-thiocytidine.Antimicrob Agents Chemother. 1999 Aug;43(8):1835-44.
- [2] Cahn P, et al. Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients.AIDS. 2006 Jun 12;20(9):1261-8.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.