[CAS NO. 348086-71-5]  Pritelivir

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PRODUCTS SPECIFICATIONS [348086-71-5]

Catalog
HY-15303
Brand
MCE
CAS
348086-71-5

DESCRIPTION [348086-71-5]

Overview

MDL-
Molecular Weight402.49
Molecular FormulaC18H18N4O3S2
SMILESO=C(N(C1=NC(C)=C(S(=O)(N)=O)S1)C)CC2=CC=C(C3=NC=CC=C3)C=C2

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


Summary

Pritelivir (AIC316), an inhibitor of the viral helicase-primase complex , exhibits antiviral activity in vitro and in animal models of herpes simplex virus ( HSV ) infection . Pritelivir 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
NCT01047540 AiCuris Anti-infective Cures AG|FHI 360
HSV-2
March 2010 Phase 2
NCT01658826 AiCuris Anti-infective Cures AG|Medpace, Inc.
Genital Herpes
October 2012 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 33 mg/mL ( 81.99 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4845 mL 12.4227 mL 24.8453 mL
5 mM 0.4969 mL 2.4845 mL 4.9691 mL
10 mM 0.2485 mL 1.2423 mL 2.4845 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Benzeneacetamide, N-[5-(aminosulfonyl)-4-methyl-2-thiazolyl]-N-methyl-4-(2-pyridinyl)-
N-[5-(Aminosulfonyl)-4-methyl-2-thiazolyl]-N-methyl-4-(2-pyridinyl)benzeneacetamide
BAY 57-1293
N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide
Pritelivir