HIV-1 inhibitor-8
Based on 1 Customer Validation
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.03%
- CAS 番号: 2826996-78-3
- 分子式: C25H21N5OS
- 分子量:439.53
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Anti-Infection Compound Library
HY-L002
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Antiviral Compound Library
HY-L027
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Orally Active Compound Library
HY-L061
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Heterocyclic Compound Library
HY-L138
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MCE Bioactive Compound Library
HY-L001V
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
生物活性
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HIV-1 (WT) 0.081 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MT4 | CC50 |
284 μM
Compound: 20a
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
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[PMID: 34432448] |
HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC50=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC50 value of 19.84 μM in CHO-hERG cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rat[1]
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Dosage:2 mg/kg
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Administration:I.v.
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Result:Showed a favorable mean CL, volume of distribution and a long terminal half-life.
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Animal Model:Sprague-Dawley (SD) rat[1]
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Dosage:20 mg/kg
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Administration:P.o.
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Result:Absorption reached maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time was 2.90 hours.
化学情報
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CAS 番号 2826996-78-3
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性状 Solid
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分子量 439.53
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分子式 C25H21N5OS
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Color Light yellow to light brown
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SMILES
N#CC1=CC=C(NC2=NC(OC3=C(C)C=C(/C=C/C#N)C=C3C)=C(CSCC4)C4=N2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 10 mg/mL (22.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wang Z, et al. Discovery of Novel Dihydrothiopyrano[4,3-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs with Significantly Reduced hERG Inhibitory Activity and Improved Resistance Profiles [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01015. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2752 mL | 11.3758 mL | 22.7516 mL | 56.8789 mL |
| 5 mM | 0.4550 mL | 2.2752 mL | 4.5503 mL | 11.3758 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2752 mL | 5.6879 mL | |
| 15 mM | 0.1517 mL | 0.7584 mL | 1.5168 mL | 3.7919 mL | |
| 20 mM | 0.1138 mL | 0.5688 mL | 1.1376 mL | 2.8439 mL |
HIV-1 inhibitor-8 関連分類
HY-132291 関連分類
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