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IQP-0528

🥰Excellent
Catalog No. T27625Cas No. 301297-45-0
Alias SJ-3991, SJ3991, IQP0528

IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.

IQP-0528

IQP-0528

🥰Excellent
Purity: 100%
Catalog No. T27625Alias SJ-3991, SJ3991, IQP0528Cas No. 301297-45-0
IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.
Pack SizePriceAvailabilityQuantity
1 mg$68In Stock
5 mg$163In Stock
10 mg$238In Stock
25 mg$403In Stock
50 mg$557In Stock
100 mg$738In Stock
200 mg$993In Stock
1 mL x 10 mM (in DMSO)$167In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.
Targets&IC50
HIV-1:0.2 nM(EC50), HIV-2:100 nM(EC50)
In vitro
The in vitro safety evaluations showed no significant loss in cell viability or significant inflammatory response after treatment with a 3.0% HEC gel containing 0.25% IQP-0528. In an in vitro HIV-1 entry inhibition assay, the lead formulation showed an 50% effective concentration of 0.14 μg/ml for gel in culture media, which corresponds to ∼0.001 μM IQP-0528.[5]
In vivo
we report the first-in-human evaluation of such a gel containing 1% IQP-0528, an investigational antiretroviral. Seven HIV-1-negative participants received one 10 mL rectal dose of radiolabeled 1% IQP-0528 gel. Median IQP-0528 concentrations in rectal tissue exceeded the in vitro EC95 against HIV-1 (0.07 ng/mg) by 3-5 h of dosing and remained above this concentration for at least 24 h, despite a 3-log reduction in concentration over this duration of time. Rectal tissue PD assessed by ex vivo HIV challenge-demonstrated significant p24 antigen reduction 3-5 h postdose compared with baseline , but not 24-26 h postdose. The IQP-0528 gel possesses desirable features for a topical microbicide including local safety with no systemic absorption, delivery of locally high IQP-0528 concentrations, and significant reductions in ex vivo HIV infectivity.[6]
AliasSJ-3991, SJ3991, IQP0528
Chemical Properties
Molecular Weight340.42
FormulaC20H24N2O3
Cas No.301297-45-0
SmilesC(=O)(C=1N(CC2CC2)C(=O)NC(=O)C1C(C)C)C3=CC(C)=CC(C)=C3
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 4 mg/mL (11.75 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9375 mL14.6877 mL29.3755 mL146.8774 mL
5 mM0.5875 mL2.9375 mL5.8751 mL29.3755 mL
10 mM0.2938 mL1.4688 mL2.9375 mL14.6877 mL

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