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Aplaviroc
🥰Excellent
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
🥰Excellent
Purity: 99.53%
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $545 | In Stock | |
| 5 mg | $1,190 | In Stock | |
| 10 mg | $1,630 | In Stock | |
| 25 mg | $2,420 | In Stock | |
| 50 mg | $3,260 | In Stock | |
| 100 mg | $4,380 | In Stock |
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Purity:99.53%
ee:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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