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Aplaviroc
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Catalog No. T14307Cas No. 461443-59-4
Alias ONO-4128, GW 873140, GSK 873140, AK 602
Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW.
Aplaviroc
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Purity: 98.26%
Catalog No. T14307Alias ONO-4128, GW 873140, GSK 873140, AK 602Cas No. 461443-59-4
Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $545 | In Stock | In Stock | |
| 5 mg | $1,190 | In Stock | In Stock | |
| 10 mg | $1,630 | In Stock | In Stock | |
| 25 mg | $2,420 | In Stock | In Stock | |
| 50 mg | $3,260 | In Stock | In Stock | |
| 100 mg | $4,380 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.26%
ee:100%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Aplaviroc (AK 602), an SDP derivative, is a CCR5 antagonist with IC50 values of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW. |
| Targets&IC50 | HIV-1 (JRFL):0.1 nM, HIV-1 (MOKW):0.2 nM, HIV-1 (Ba-L):0.4 nM |
| In vitro | Aplaviroc showed an IC50 value of 0.1 to 0.4 nM for the three wild-type R5 HIV-1 strains (HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW) and effectively blocked rgp120/sCD4 and CCR5 with an IC50 value of 2.7 nM; Aplaviroc inhibited the infectivity and replication of the two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at very low concentrations (IC50 value 0.4 to 0.6 nM), while the two R5 HIV-1 variants inhibited zidovudine, nelfinavir, and nafenacil. Aplaviroc inhibits the infectivity and replication of the two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at very low concentrations (IC50 values of 0.4 to 0.6 nM), resulting in AplavirocKd values of 2.9±1.0 nM, respectively; Aplaviroc's potent activity against R5 HIV-1 stems from its high-affinity binding to ECL2B and/or its neighboring regions, which leads to inhibition of the interaction between rgp120/CD4 and CCR5. gp120/CD4 binding to CCR5 [1]. |
| In vivo | The concentration of apraviroc (AK602) reaches maximum concentration immediately after intraperitoneal administration and decreases rapidly [2];Aplaviroc (AK602, 60 mg/kg, bid, daily) inhibits R5 HIV-1 viremia in hu-PBMC-NOG mice[2]. |
| Synonyms | ONO-4128, GW 873140, GSK 873140, AK 602 |
| Molecular Weight | 577.71 |
| Formula | C33H43N3O6 |
| Cas No. | 461443-59-4 |
| Smiles | C(CCC)N1C2(C(=O)N[C@]([C@H](O)C3CCCCC3)(C1=O)[H])CCN(CC4=CC=C(OC5=CC=C(C(O)=O)C=C5)C=C4)CC2 |
| Relative Density. | 1.29 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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