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VX-765

Cat. No. M3532
VX-765 Structure
Size Price Availability Quantity
5mg USD 75 In stock
10mg USD 100 In stock
50mg USD 330 In stock
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Quality Control
Biological Activity

VX-765 is a novel and irreversible IL-converting enzyme/caspase-1 inhibitor with an IC50 of 0.8 nM. VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases is an active metabolite VX-765. VRT-043198 exhibits 100-10,000-fold selectivity against other caspase-3 and -6-9. VX-765 was efficiently converted to VRT-043198 when administered orally to mice and inhibited LPS-induced cytokine secretion. VX-765 has been shown to inhibit acute partial seizures in preclinical models and has shown activity in preclinical models of chronic partial epilepsy that do not respond to currently available medicines for epilepsy. In addition, VX-765 reduced disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Collagen-Induced Arthritis Model in Mouse
Formulation 25% Cremophor EL
Dosages 10-100 mg/kg twice daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 509
Formula C24H33ClN4O6
CAS Number 273404-37-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Brain Behav Immun (2016). Figure 7. VX-765
Method i.v.
Cell Lines C57BL/6 mice
Concentrations 25 mg/kg/day and 50 mg/kg/day
Incubation Time four weeks
Results As shown in Fig. 7A–B, with administration of VX-765 (25 mg/kg/day and 50 mg/kg/day), the mice showed decreased levels of mature IL-1b and IL-18 as compared to those with vehicle treatment (P < 0.01).
Rating
Source Brain Behav Immun (2016). Figure 6. VX-765
Method i.v.
Cell Lines C57BL/6 mice
Concentrations 50 mg/kg/day
Incubation Time four weeks
Results Administration of VX-765 ameliorated depression- and anxiety-like behavior in OVX mice. VX-765 (50 mg/kg/day) significantly increased percentage of sucrose consumption in OVX mice as compared to vehicletreated OVX group.
Rating
References

(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.
Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16. PMID: 17289835.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: VX-765 supplier, Caspase, inhibitors

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