| BAY 57-1293HSV helicase-primase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.24%
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| Cas No. | 348086-71-5 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)-2-(4-pyridin-2-ylphenyl)acetamide | ||
| Canonical SMILES | CC1=C(SC(=N1)N(C)C(=O)CC2=CC=C(C=C2)C3=CC=CC=N3)S(=O)(=O)N | ||
| Formula | C18H18N4O3S2 | M.Wt | 402.49 |
| Solubility | ≥13.9mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
BAY 57-1293 is a potent and safe inhibitor of HSV helicase-primase with IC50 value of 12nM [1].
BAY 57-1293 displays anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. In the plaque reduction assay and the conventional cytopathogenicity assay, BAY 57-1293 shows IC50 values of 0.01-0.02μM and 0.01-0.03μM, respectively. Besides that, BAY 57-1293 is active at an IC50 value of 10nM–30nM against all clinical isolates of HSV-1 and HSV-2. Furthermore, BAY 57-1293 is active in vivo. The oral administration of BAY 57-1293 shows 10-fold more potent than valacyclovir in a murine model of disseminated herpes infection. In a rat lethal challenge model, BAY 57-1293 exerts profound antiviral activity without toxic effects. [1, 2]
References:[1] Kleymann G, Fischer R, Betz U A K, et al. New helicase-primase inhibitors as drug candidates for the treatment of herpes simplex disease. Nature medicine, 2002, 8(4): 392-398.[2] Betz U A K, Fischer R, Kleymann G, et al. Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293. Antimicrobial agents and chemotherapy, 2002, 46(6): 1766-1772.
