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

VRT-043198, the agent 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.

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VRT-043198 Chemical Structure

VRT-043198 Chemical Structure

CAS No. : 244133-31-1

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

VRT-043198 Related Antibodies

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  • Purity & Documentation

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Description

VRT-043198, the agent 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].

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

VRT-043198 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C=O)CC(O)=O)[C@H]1N(C([C@H](C(C)(C)C)NC(C2=CC=C(N)C(Cl)=C2)=O)=O)CCC1
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 : 100 mg/mL (207.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of 4.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0793 mL 10.3963 mL 20.7926 mL 51.9815 mL
5 mM 0.4159 mL 2.0793 mL 4.1585 mL 10.3963 mL
10 mM 0.2079 mL 1.0396 mL 2.0793 mL 5.1982 mL
15 mM 0.1386 mL 0.6931 mL 1.3862 mL 3.4654 mL
20 mM 0.1040 mL 0.5198 mL 1.0396 mL 2.5991 mL
25 mM 0.0832 mL 0.4159 mL 0.8317 mL 2.0793 mL
30 mM 0.0693 mL 0.3465 mL 0.6931 mL 1.7327 mL
40 mM 0.0520 mL 0.2599 mL 0.5198 mL 1.2995 mL
50 mM 0.0416 mL 0.2079 mL 0.4159 mL 1.0396 mL
60 mM 0.0347 mL 0.1733 mL 0.3465 mL 0.8664 mL
80 mM 0.0260 mL 0.1300 mL 0.2599 mL 0.6498 mL
100 mM 0.0208 mL 0.1040 mL 0.2079 mL 0.5198 mL
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VRT-043198 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VRT-043198244133-31-1VRT043198VRT 043198CaspaseDrug MetabolitelipopolysaccharideLPScytokinerheumatoidarthritisIL-1βICEInhibitorinhibitorinhibit

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