Belnacasan (VX-765)
Catalog No.S2228
Molecular Weight(MW): 509
Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.
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(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
Cell, 2018, 175(2):442-457. Belnacasan (VX-765) purchased from Selleck.
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BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control.
Mucosal Immunol, 2015, 10.1038/mi.2015.44. Belnacasan (VX-765) purchased from Selleck.
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(c,d) HMDMs and BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control. Similar results were obtained in two independent experiments. Ctrl, control; DMSO, dimethyl sulfoxide.
Mucosal Immunol, 2016, 9(1):124-36. Belnacasan (VX-765) purchased from Selleck.
(A) LPS-primed J774A.1 macrophages were treated with DCA (100 μM) in the presence or absence of caspase-1 inhibitor belnacasan (10 μM). IL-1β in supernatants was analyzed by ELISA.
Front Immunol, 2016, 7:536.. Belnacasan (VX-765) purchased from Selleck.
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(A, B and C) Quantitative real‐time PCR for the transcript expression levels of matrix metalloproteinases 3, matrix metalloproteinases 13 and COL2A1 in NP cells after treatment with AGEs‐BSA (100 μg/ml) or recombinant human IL‐1β (1 ng/ml) for 48 hrs, combined with si‐NLRP3, VX‐765 and IL‐1Ra or not. Data were presented as mean ± S.D. (n = 3). *P < 0.05 versus control, #P < 0.05 versus AGEs‐BSA + si‐control, &P < 0.05 versus IL‐1β.
J Cell Mol Med, 2017, 21(7):1373-1387. Belnacasan (VX-765) purchased from Selleck.
Purity & Quality Control
Choose Selective Caspase Inhibitors
Biological Activity
| Description | Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2. | ||||
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| Features | A potent and selective inhibitor of interleukin-converting enzyme/caspase-1. | ||||
| Targets |
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| In vitro |
VX-765 is an orally absorbed prodrug of VRT-043198, which exhibits potent inhibition against ICE/caspase-1 and caspase-4 with Ki of 0.8 nM and less than 0.6 nM, respectively. And VRT-043198 also inhibits IL-1β release from both PBMCs and whole blood with IC50 of 0.67 μM and 1.9 μM, respectively. [1] |
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| In vivo | In collagen-induced arthritis mouse model, VX-765 (200 mg/kg) inhibits LPS-induced IL-1β production by about 60%, and results in a dose-dependent, statistically significant reduction in the inflammation scores and effective protection from joint changes. [1] In vivo, VX-765 blocks kindling epileptogenesis in rats by preventing IL-1β increase in forebrain astrocytes without significant effect on afterdischarge duration. [2] In the mouse model of acute seizures, VX-765 (50 mg/kg-200 mg/kg) produces the anticonvulsant effect by delaying the time to onset of the first seizure and decreasing the number of seizures as well as their total duration by average 50% and 64%. [3] In adult rats with genetic absence epilepsy (GAERS), VX-765, after the 3rd drug injection, significantly reduces the cumulative duration and number of spike-and-wave discharges (SWDs) by 55% on average by selectively blocking IL-1β biosynthesis. [4] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL warmed (196.46 mM) |
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| Ethanol | 100 mg/mL warmed (196.46 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 509 |
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| Formula | C24H33ClN4O6 |
| CAS No. | 273404-37-8 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01501383 | Terminated | Epilepsy | Vertex Pharmaceuticals Incorporated | December 2011 | Phase 2 |
| NCT01501383 | Terminated | Epilepsy | Vertex Pharmaceuticals Incorporated | December 2011 | Phase 2 |
| NCT01048255 | Completed | Partial Epilepsy | Vertex Pharmaceuticals Incorporated | January 2010 | Phase 2 |
| NCT01048255 | Completed | Partial Epilepsy | Vertex Pharmaceuticals Incorporated | January 2010 | Phase 2 |
| NCT00205465 | Completed | Psoriasis | Vertex Pharmaceuticals Incorporated | December 2004 | Phase 2 |
| NCT00205465 | Completed | Psoriasis | Vertex Pharmaceuticals Incorporated | December 2004 | Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
The recommended dose of VX-765 is 100mg/kg p.o. in 25% cremophor EL in water. Is VX0765 directly soluble at 10mg/ml in 25% cremophor in water? How to formulate it for in vivo use in mice?
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Answer:
You can prepare 25% cremophor EL in water first and then directly resuspend VX-765 powder in the vehicle. The powder may not be fully dissolved, but the suspension is stable and can be used for gavage feeding.
