Product Details
Product Name:
IQP-0528 |
CAS No.:
301297-45-0 |
Purity:
98.40% |
Supply Ability:
10g |
Release date:
2024/11/08 |
Product Introduction
Bioactivity
名稱 | IQP-0528 |
描述 | 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. |
體外活性 | 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] |
體內(nèi)活性 | 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] |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 4 mg/mL (11.75 mM)
|
關(guān)鍵字 | SJ 3991 | IQP 0528 | IQP-0528 |
相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Inosine pranobex | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 4500-5500) | Lamivudine | Chloroquine phosphate | Tenofovir Disoproxil Fumarate | Decanedioic acid | Tenofovir |
相關(guān)庫 | 經(jīng)典已知活性庫 | 抗病毒庫 | 抑制劑庫 | 已知活性化合物庫 |
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 |
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |