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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3033486-43-7
- Formule: C24H18F3N5O3
- Masse moléculaire:481.43
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Stockage:
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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Activité biologique
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Chemical Information
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Activité biologique
Description
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 |
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| 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] |
In Vitro
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.
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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.
In Vivo
| 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.
Chemical Information
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CAS No. 3033486-43-7
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Masse moléculaire 481.43
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZLM-66 Related Classifications
HY-150769 Related Classifications
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