SGC-NSP2hel-1
SGC-NSP2hel-1 (RA-0188293), a chemical probe, is a potent, specific and orally active nsP2 inhibitor. SGC-NSP2hel-1 has broad spectrum activity against multiple alphaviruses of the nsP2 helicase with a CC50 > 250 μM. SGC-NSP2hel-1 (RA-0188293) shows selectivity index > 4000 against human RNA helicases. SGC-NSP2hel-1 reduces virus replication and limited virus-induced pathology by forming a stable complex with nsP2 and ATP in a preclinical small animal model of CHIKV disease.
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- Fòrmula: C26H38N2O4S
- Peso molecular:474.66
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Helicase |
SGC-NSP2hel-1 (3 days) inhibits multiple alphaviruses with very little impact on cell viability with a CC50 > 250 µM and Selectivity Index of > 4000 in MRC-5 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Mice | 10 mg/kg | i.p. | 0.347863436 h | 1145 ng/mL |
| Mice | 10 mg/kg | p.o. | 0.298279779 h | 7.81 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CHIKV models of 6-week mice[1]
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Dosage:30 mg/kg
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Administration:Orally twice daily and once daily with 100mg/kg 1-ABT, beginning at 12 h prior to infection with CHIKV.
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Result:Significantly reduced footpad swelling and virus replication in the ipsilateral foot and serum.
Significantly decreased virus-induced pathology, with decreased inflammatory cell recruitment and reduced myositis and muscle damage.
Showed no apparent toxicity (body weight and H&E staining).
Chemical Information
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Peso molecular 474.66
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Fòrmula C26H38N2O4S
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SMILES
O=C(C1(CCCC1)C2=CC=CC=C2)N(CC3)CCC43OCC[C@@H](CN5CCCCS5(=O)=O)C4
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Synonyms
RA-0188293; RA-NSP2-1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SGC-NSP2hel-1 Related Classifications
HY-176268 Related Classifications
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