ZLM-66
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS.
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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。
- CAS 番号: 3033486-43-7
- 分子式: C24H18F3N5O3
- 分子量:481.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
HIV-1 (WT) 13 nM (EC50) |
HIV-1 (K103N) 13 nM (EC50) |
HIV-1 (L100I) 24 nM (EC50) |
HIV-1 (E138K) 25 nM (EC50) |
HIV-1 (Y181C) 58 nM (EC50) |
HIV-1 (K103N+Y181C) 260 nM (EC50) |
HIV-1 (F227L+V106A) 27530 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
26.45 μM
Compound: B3; ZLM-66
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Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
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[PMID: 35797898] |
体外実験
ZLM-66 (0.0016-125 μg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MT-4 cells infected with WT HIV-1 strain (IIIB) or HIV-2 (ROD)
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Concentration:125, 25, 5, 1, 0.2, 0.04, 0.008 and 0.0016 µg/ml
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Incubation Time:5 d
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Result:Exbited EC50 value, CC50 value and SI value of 13 nM, 26.45 μM and 2019.8 respectively against HIV-1 (IIIB). Inhibited L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, and K103N + Y181C (single and double HIV mutant strains) with EC50s of 24, 13, 58, 760, 25, 27530 and 260 nM, respectively.
体内実験
| Rat IV 1 mg/kg |
Rat PO 5 mg/kg |
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| T1/2 (h) | 1.90±0.28 | 8.45±4.88 |
| Tmax (h) | 0.08±0.00 | 6.67±1.15 |
| Cmax (ng/mL) | 468.67±63.09 | 583.33±290.11 |
| AUC0-t (h*ng/ml) | 891.94±79.30 | 4983.22±3220.11 |
| AUC0-∞ (h*ng/ml) | 940.41±105.00 | 6594.05±1547.74 |
| CL (ml/h/kg) | 1072.31±120.40 | 791.14±210.66 | /tr>
| MRT0-t (h) | 2.03±0.2 | 6.79±1.90 | /tr>
| MRT0-∞ (h) | 2.48±0.35 | 13.92±6.44 |
| F (%) | 140.24 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six- to 8-week-old male Sprague-Dawley rats (180−230 g)[1]
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Dosage:1, 5 mg/kg
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Administration:Intravenous injection, oral gavage; 1-5 mg/kg; once
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Result:Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.
化学情報
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CAS 番号 3033486-43-7
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分子量 481.43
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分子式 C24H18F3N5O3
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SMILES
CN1C(CN(C=CC(C(F)(F)F)=C2OC3=CC(C#N)=CC(C4=CC(C)=CC=C4)=C3)C2=O)=NNC1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ZLM-66 関連分類
HY-150769 関連分類
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