VRT-043198
Based on 5 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 97.66%
- CAS. Nr.: 244133-31-1
- Formel: C22H29ClN4O6
- Molecular Weight:480.94
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) VRT-043198
MoreAlle Caspase Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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Caspase-1 0.8 nM (Ki) |
Caspase-4 0.6 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| PBMC | IC50 |
0.47 μM
Compound: VRT-043198
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Inhibition of LPS-induced IL-1beta release in PBMC (unknown origin)
Inhibition of LPS-induced IL-1beta release in PBMC (unknown origin)
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[PMID: 34823899] |
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.
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.
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Animal Model:Naïve male CD-1 mice[1].
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Dosage:25-200 mg/kg.
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Administration:Oral gavage 1 h before i.v. injection of 2 mg/kg E. coli LPS (strain 0111:B4).
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Result:Reduced serum IL-1β levels.
Chemical Information
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CAS. Nr. 244133-31-1
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Appearance Solid
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Molecular Weight 480.94
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Formel C22H29ClN4O6
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Color White to off-white
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Chemotherapy-induced activation of caspase-1 and IL-1α release by cancer cells remotely skews myelopoiesis to drive pro tumorigenic systemic neutrophil-dominant inflammation. [Abstract]2026 Apr 20;17(1):4724. PMID: 42009646 -
JACS Au
Mapping the Binding Interactions between Human Gasdermin D and Human Caspase-1 Using Carbene Footprinting. [Abstract]2023 Jun 23;3(7):2025-2035. PMID: 37502151 -
J Oral Microbiol
Recognition of Porphyromonas gingivalis lipopolysaccharide by human caspase-4 depends on lipopolysaccharide purity and guanylate-binding protein 1. [Abstract]2025 Dec 1;17(1):2589652. PMID: 41341206 -
Neuropsychiatr Dis Treat
VRT-043198 Ameliorates Surgery-Induced Neurocognitive Disorders by Restoring the NGF and BNDF Expression in Aged Mice. [Abstract]2022 May 16:18:1027-1037. PMID: 35607505 -
bioRxiv
Multimodal profiling of proinflammatory protease activity identifies caspase-1 as a target for lung cancer interception. [Abstract]2025 Jul 2:2025.07.01.662195. PMID: 40631193
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Woods Wannamaker, et al. (S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18. J Pharmacol Exp Ther. 2007 May;321(2):509-16. [Content Brief]
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 |
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| 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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