1. Apoptosis
    Metabolic Enzyme/Protease
  2. Caspase
    Drug Metabolite
  3. VRT-043198

VRT-043198 

Cat. No.: HY-112226 Purity: 98.05%
Handling Instructions

VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.

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

VRT-043198 Chemical Structure

VRT-043198 Chemical Structure

CAS No. : 244133-31-1

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Based on 1 publication(s) in Google Scholar

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Description

VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively[1].

IC50 & Target[1]

Caspase-1

0.8 nM (Ki)

Caspase-4

0.6 nM (Ki)

In Vitro

VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9[1].
VRT043198 inhibits the release of interleukin (IL)-1β and IL-18, but it has little effect on the release of several other cytokines, including IL-1α, tumor necrosis factor-, IL-6 and IL-8. VRT-043198 inhibited IL-1β release from both PBMCs (n = 8) and whole blood (n = 4) with IC50 values of 0.67±0.55 and 1.9±0.80 nM, respectively[1].
VRT-043198 lacks potent antiapoptotic activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases and also much more slowly in aqueous solution[1].
VX765 reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation[1].
VX765 (25, 50, 100, or 200 mg/kg) inhibits lipopolysaccharide-induced cytokine secretion[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Naïve male CD-1 mice[1].
Dosage: 25-200 mg/kg.
Administration: Oral gavage 1 h before i.v. injection of 2 mg/kg E. coli LPS (strain 0111:B4).
Result: Reduced serum IL-1β levels.
Molecular Weight

480.94

Formula

C₂₂H₂₉ClN₄O₆

CAS No.
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 : 180 mg/mL (374.27 mM; Need ultrasonic)

Methanol : 12.5 mg/mL (25.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0793 mL 10.3963 mL 20.7926 mL
5 mM 0.4159 mL 2.0793 mL 4.1585 mL
10 mM 0.2079 mL 1.0396 mL 2.0793 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: 4.5 mg/mL (9.36 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 4.5 mg/mL (9.36 mM); Clear solution

  • 3.

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

    Solubility: ≥ 4.5 mg/mL (9.36 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
VRT-043198
Cat. No.:
HY-112226
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