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IQP-0528

Catalog No. T27625 CAS 301297-45-0

Synonyms: 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.

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IQP-0528, CAS 301297-45-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 133.00
5 mg	In stock	$ 320.00
10 mg	In stock	$ 480.00
25 mg	In stock	$ 786.00
50 mg	In stock	$ 1,080.00
100 mg	In stock	$ 1,480.00
500 mg	In stock	$ 2,960.00
1 mL * 10 mM (in DMSO)	In stock	$ 328.00

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Purity: 100%

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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]

Synonyms	SJ-3991, SJ3991, IQP0528
Molecular Weight	340.42
Formula	C20H24N2O3
CAS No.	301297-45-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4 mg/mL (11.75 mM)

References and Literature

1. Su JT, et al. A Dose Ranging Pharmacokinetic Evaluation of IQP-0528 Released from Intravaginal Rings in Non-Human Primates. Pharm Res. 2017;34(10):2163-2171. 2. Pereira LE, et al. Pharmacokinetic and Pharmacodynamic Evaluation following Vaginal Application of IQB3002, a Dual-Chamber Microbicide Gel Containing the Nonnucleoside Reverse Transcriptase Inhibitor IQP-0528 in Rhesus Macaques. Antimicrob Agents Chemother. 2015;60(3):1393-1400. 3. Srinivasan P, et al. Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis. Antimicrob Agents Chemother. 2016;60(7):4140-4150. 4. Dezzutti CS, et al. Safety and efficacy of tenofovir/IQP-0528 combination gels - a dual compartment microbicide for HIV-1 prevention. Antiviral Res. 2012;96(2):221-225. 5. Ham AS, et al. Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection. Pharm Res. 2012;29(7):1897-1907. 6. Mahalingam A, et al. Vaginal microbicide gel for delivery of IQP-0528, a pyrimidinedione analog with a dual mechanism of action against HIV-1. Antimicrob Agents Chemother. 2011;55(4):1650-1660. 7. Al-Khouja A, et al. Examining the Safety, Pharmacokinetics, and Pharmacodynamics of a Rectally Administered IQP-0528 Gel for HIV Pre-Exposure Prophylaxis: A First-In-Human Study. AIDS Res Hum Retroviruses. 2021;37(6):444-452.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Viral Compound Library

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Keywords

IQP-0528 301297-45-0 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome Antiviral HIV Protease Reverse Transcriptase SJ 3991 IQP 0528 SJ-3991 SJ3991 IQP0528 inhibitor inhibit

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