AVG-233
Based on 1 Customer Validation
AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV).
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- Pureté: 98.13%
- CAS No.: 2151937-80-1
- Formule: C26H22ClN5O3
- Masse moléculaire:487.94
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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RNA Polymerase |
AVG-233 (1-100 μM) blocks 3′RNA extension elongation but does not interfere with 3′RNA extension by up to three nucleotides after de novo initiation from the promoter or back-priming[1].
AVG-233 (20 μM) reduces virus yield of RSV A2-L19F (EC50=0.31 μM), RSV strain 2-20 (EC50=0.14 μM) and RSV clinical isolate 718 (EC50=0.2 μM) [1].
AVG-233 (1.25-40 μM; 0-300 s) suppresses RNA synthesis by the L1-1749 fragment in a dose-dependent manner with an IC50 value of 13.7 μM. AVG-233 bounds L and the L1-1749 fragment with similar affinities (dissociation constants (KD’s) are 38.3 μM and 53.1 μM, respectively)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AVG-233 (2-20 mg/kg; i.v. and p.o.; once; male CD-1 mice) has good orally bioavailable and the maximum plasma concentration about 2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/cJ mice with recRSV-mKate xenograft[2]
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Dosage:50 and 100 mg/kg
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Administration:Oral gavage; once
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Result:Reduced in lung viral load of 0.89 log10 TCID50 (median tissue culture infectious dose)/mL.
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Animal Model:Male CD-1 mice (27-29 g)[1]
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Dosage:2 mg/kg (i.v.) and 20 mg/kg (p.o.)
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Administration:Intravenous injection and oral administration; once, obtains blood samples at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h post-dosing
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Result:
1.19 Route Dose Tmax Cmax AUC0-∞ CL/F T1/2 Bioavailability mg/kg h nmol/ml h×nmol/ml liters/h/kg h % Oral 20 1 2.17 5.95 6.98 5.28 33.8
Chemical Information
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CAS No. 2151937-80-1
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Appearance Solid
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Masse moléculaire 487.94
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Formule C26H22ClN5O3
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Color Off-white to yellow
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SMILES
O=C1N(C2=NC=CC=C2)N(CC3=CC=C(OC)C=C3)C(C1=C(C)N4CC5=NC(Cl)=CC=C5)=CC4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 50 mg/mL (102.47 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Cox RM, et, al. Development of an allosteric inhibitor class blocking RNA elongation by the respiratory syncytial virus polymerase complex. J Biol Chem. 2018 Oct 26;293(43):16761-16777. [Content Brief]
[2]. Sourimant J, et, al. Orally efficacious lead of the AVG inhibitor series targeting a dynamic interface in the respiratory syncytial virus polymerase. Sci Adv. 2022 Jun 24;8(25):eabo2236. [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 (sealed storage, away from moisture and light). 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 | 2.0494 mL | 10.2472 mL | 20.4943 mL | 51.2358 mL |
| 5 mM | 0.4099 mL | 2.0494 mL | 4.0989 mL | 10.2472 mL | |
| 10 mM | 0.2049 mL | 1.0247 mL | 2.0494 mL | 5.1236 mL | |
| 15 mM | 0.1366 mL | 0.6831 mL | 1.3663 mL | 3.4157 mL | |
| 20 mM | 0.1025 mL | 0.5124 mL | 1.0247 mL | 2.5618 mL | |
| 25 mM | 0.0820 mL | 0.4099 mL | 0.8198 mL | 2.0494 mL | |
| 30 mM | 0.0683 mL | 0.3416 mL | 0.6831 mL | 1.7079 mL | |
| 40 mM | 0.0512 mL | 0.2562 mL | 0.5124 mL | 1.2809 mL | |
| 50 mM | 0.0410 mL | 0.2049 mL | 0.4099 mL | 1.0247 mL | |
| 60 mM | 0.0342 mL | 0.1708 mL | 0.3416 mL | 0.8539 mL | |
| 80 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6404 mL | |
| 100 mM | 0.0205 mL | 0.1025 mL | 0.2049 mL | 0.5124 mL |
AVG-233 Related Classifications
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