[CAS NO. 2151937-80-1]  AVG-233

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PRODUCTS SPECIFICATIONS [2151937-80-1]

Catalog
HY-122587
Brand
MCE
CAS
2151937-80-1

DESCRIPTION [2151937-80-1]

Overview

MDL-
Molecular Weight487.94
Molecular FormulaC26H22ClN5O3
SMILESO=C1N(C2=NC=CC=C2)N(CC3=CC=C(OC)C=C3)C(C1=C(C)N4CC5=NC(Cl)=CC=C5)=CC4=O

For research use only. We do not sell to patients.

Summary

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 L 1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates ( EC 50 =0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV) [1] [2] .


In Vitro

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 (EC 50 =0.31 μM), RSV strain 2-20 (EC 50 =0.14 μM) and RSV clinical isolate 718 (EC 50 =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 IC 50 value of 13.7 μM. AVG-233 bounds L and the L 1-1749 fragment with similar affinities (dissociation constants (KD’s) are 38.3 μM and 53.1 μM, respectively) [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

AVG-233 (50-100 mg/kg; i.g.; once) decreases lung viral load in the RSV mouse model [2] .
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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Balb/cJ mice with recRSV-mKate xenograft [2]
Dosage: 50 and 100 mg/kg
Administration: Oral gavage; once
Result: Reduced in lung viral load of 0.89 log 10 TCID 50 (median tissue culture infectious dose)/mL.
Animal Model: Male CD-1 mice (27-29 g) [1]
Dosage: 2 mg/kg (i.v.) and 20 mg/kg (p.o.)
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
Result: 1.19
Route Dose T max C max AUC 0-∞ CL/F T 1/2 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

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

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)