Product Details
Product Name:
Apricitabine |
CAS No.:
160707-69-7 |
Purity:
100% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | Apricitabine |
Description | Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance. |
In vitro | Apricitabine (SPD754 ; AVX754) is against clinical isolates of HIV-1 in cultured?PBMCs with IC50 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 against HIV-1 clinical isolates resistant to nucleoside reverse transcriptase inhibitors in MT-4 cells, exhibits Mean IC50 values of 20 μM, 25 μM, 30 μM,21 μM,55 μM,32 μM and 71 μM. It is for HIV-1IIIB, Wild-type(control), Zidovudine-resistant/lamivudine-resistant, Zidovudine-resistant, Lamivudine-resistant, Abacavir-resistant and Stavudine-resistant viruses, respectively.[2] |
In vivo | Apricitabine (SPD754 ; AVX754) (intravenous?injection ; 10 mg/kg ; once a day) exhibits the T1/2, AUC0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats[1]. 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 T1/2, AUC0–∞, Tmax, Cmax are 62.2 mins, 157.4 μg/min/ml and 37.3 mins, 1.16 μg/ml in female rats.[1] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 11 mg/mL (47.98 mM)
|
Keywords | Apricitabine | SPD-754 | SPD 754 | AVX 754 | AVX-754 |
Inhibitors Related | Stavudine | Rifampicin | 5-Fluorouracil | Emtricitabine | Dextran sulfate sodium salt (MW 4500-5500) | Guanidine hydrochloride | Lamivudine | Thymidine | Decanedioic acid |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$314.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |