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[CAS NO. 1428333-96-3] Pritelivirmesylate
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15303A |
| Brand: | MCE |
| CAS: | 1428333-96-3 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 498.60 |
| Molecular Formula | C19H22N4O6S3 |
| SMILES | O=C(N(C1=NC(C)=C(S(=O)(N)=O)S1)C)CC2=CC=C(C3=NC=CC=C3)C=C2.OS(=O)(C)=O |
2 Publications Citing Use of MCE
Summary
Pritelivir mesylate (BAY 57-1293 mesylate), an inhibitor of the viral helicase-primase complex , exhibits antiviral activity in vitro and in animal models of herpes simplex virus ( HSV ) infection . Pritelivir mesylate is active against herpes simplex virus types 1 and 2 ( HSV-1 and HSV-2 ) with the IC 50 of 0.02 μM against HSV1-2 [1] .
IC50 & Target
|
HSV-1 0.02 μM (IC 50 ) |
HSV-2 0.02 μM (IC 50 ) |
In Vivo
Pritelivir is the first in a class of antiviral agents that inhibit HSV replication by targeting the viral helicase–primase enzyme complex
[2]
.
Pritelivir (0.03-45 mg/kg) significantly increases survival. Pritelivir (0.3-30 mg/kg) reduces mortality against HSV-1, E-377. Pritelivir 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
[3]
.
Combination therapies of Pritelivir 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
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female BALB/c mice [3] |
| Dosage: | 0.03 to 45 mg/kg |
| Administration: | Administered orally, twice daily at approximately 12 h intervals, for 7 days |
| Result: | Survival was significantly increased to 80-100% as compared to the vehicle treatment. Even the lowest dose of 0.3 mg/kg was effective in increasing survival to 53%. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02871492 | AiCuris Anti-infective Cures AG|Novella Clinical |
Herpes Labialis
|
November 29, 2016 | Phase 2 |
| NCT03073967 | AiCuris Anti-infective Cures AG|Medpace, Inc. |
HSV Infection
|
May 8, 2017 | Phase 3 |
| NCT01658826 | AiCuris Anti-infective Cures AG|Medpace, Inc. |
Genital Herpes
|
October 2012 | Phase 2 |
| NCT05513625 | AiCuris Anti-infective Cures AG |
HSV Infection
|
July 13, 2020 | Phase 1 |
| NCT01047540 | AiCuris Anti-infective Cures AG|FHI 360 |
HSV-2
|
March 2010 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 83.33 mg/mL ( 167.13 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0056 mL | 10.0281 mL | 20.0562 mL |
| 5 mM | 0.4011 mL | 2.0056 mL | 4.0112 mL |
| 10 mM | 0.2006 mL | 1.0028 mL | 2.0056 mL |
References
- [1] Ligat G, et al. Identification of Amino Acids Essential for Viral Replication in the HCMV Helicase-PrimaseComplex. Front Microbiol. 2018 Oct 23;9:2483.
- [2] Wald A, et al. Helicase-primase inhibitor Pritelivir for HSV-2 infection. N Engl J Med. 2014 Jan 16;370(3):201-10.
- [3] Quenelle DC, et al. Efficacy of pritelivir and acyclovir in the treatment of herpes simplex virus infections in a mouse model of herpes simplex encephalitis. Antiviral Res. 2018 Jan;149:1-6.
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