BAY-57-1293


Catalog No. size PriceQuantity
M6482-2 2mg solid $77
M6482-10 10mg solid $324

Description

BAY-57-1293 is a potent helicase primase inhibitor. BAY-57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY-57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations.

Product information

CAS Number: 348086-71-5

Molecular Weight: 402.49

Formula: C18H18N4O3S2

Synonym:

BAY-571293

AIC-316

Pritelivir

Chemical Name: N-methyl-N-(4-methyl-5-sulfamoylthiazol-2-yl)-2-(4-(pyridin-2-yl)phenyl)acetamide

Smiles: CC1N=C(SC=1S(N)(=O)=O)N(C)C(=O)CC1=CC=C(C=C1)C1=CC=CC=N1

InChiKey: IVZKZONQVYTCKC-UHFFFAOYSA-N

InChi: InChI=1S/C18H18N4O3S2/c1-12-17(27(19,24)25)26-18(21-12)22(2)16(23)11-13-6-8-14(9-7-13)15-5-3-4-10-20-15/h3-10H,11H2,1-2H3,(H2,19,24,25)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vivo:

BAY-57-1293 is the first in a class of antiviral agents that inhibit HSV replication by targeting the viral helicase-primase enzyme complex. BAY-57-1293 (0.03-45 mg/kg) significantly increases survival. BAY-57-1293 (0.3-30 mg/kg) reduces mortality against HSV-1, E-377. BAY-57-1293 has potent and resistance-breaking antiviral efficacy with potential for the treatment of potentially life-threatening HSV type 1 and 2 infections, including herpes simplex encephalitis. Combination therapies of BAY-57-1293 at 0.1 or 0.3 mg/kg/dose with Acyclovir (10 mg/kg/dose) are protective when compared to the vehicle treated group against HSV-2, strain MS.

References:

  1. Burrel S, Rouard C, Boutolleau D. Helicase-primase inhibitor pritelivir for HSV-2 infection. N Engl J Med. 2014 Apr 24;370(17):1663-4. doi: 10.1056/NEJMc1402071. PubMed PMID: 24758629.
  2. Edlefsen PT, Birkmann A, Huang ML, Magaret CA, Kee JJ, Diem K, Goldner T, Timmler B, Stoelben S, Ruebsamen-Schaeff H, Zimmermann H, Warren T, Wald A, Corey L. No Evidence of Pritelivir Resistance Among Herpes Simplex Virus Type 2 Isolates After 4 Weeks of Daily Therapy. J Infect Dis. 2016 Jul 15;214(2):258-64. doi: 10.1093/infdis/jiw129. Epub 2016 Apr 7. PubMed PMID: 27056950; PubMed Central PMCID: PMC4918824.
  3. Wald A, Timmler B, Magaret A, Warren T, Tyring S, Johnston C, Fife K, Selke S, Huang ML, Stobernack HP, Zimmermann H, Corey L, Birkmann A, Ruebsamen-Schaeff H. Effect of Pritelivir Compared With Valacyclovir on Genital HSV-2 Shedding in Patients With Frequent Recurrences: A Randomized Clinical Trial. JAMA. 2016 Dec 20;316(23):2495-2503. doi: 10.1001/jama.2016.18189. Erratum in: JAMA. 2017 Feb 14;317(6):648. PubMed PMID: 27997653.

Products are for research use only. Not for human use.

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