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VX-765 (Belnacasan)

Cat. No. M3532
VX-765 (Belnacasan) Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 62  USD62 In stock
5mg USD 55  USD55 In stock
10mg USD 90  USD90 In stock
50mg USD 275  USD275 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.

Product Citations
Customer Product Validations & Biological Datas
Source EMBO Mol Med (2020 Jan). Figure 6. VX-765 (AbMole BioScience, Houston, TX, USA)
Method intraperitoneal injections
Cell Lines male GPx8-/- mice
Concentrations 20 mg/kg
Incubation Time 14 days
Results Consistently, VX-765 treatment was also associated with lower mortality and less disease severity in mice with DSS-induced colitis.
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).
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.
Cell Experiment
Cell lines human PBMCs
Preparation method A total of 2×105 cells/well (100 μL cell suspension) is distributed in triplicate in flat-bottom 96-well plates. Either 50 μL of Belnacasan (40 μM in RPMI 1640 complete medium containing 0.2% DMSO) or vehicle control is added to appropriate wells. Following a 30-min incubation at 37°C, 50 μL of LPS diluted in RPMI 1640 complete medium is added at final concentrations varying from 0.001 to 10 ng/mL. Cells are returned to a 37°C incubator. At 4 h after LPS addition, 75 μL of supernatant is removed from wells, cleared by centrifugation for 5 min at 1500 rpm, and stored at 4°C until assayed. Cells are returned to a 37°C incubator until 24 h after LPS addition, at which time 100 μL of supernatant is removed, cleared by centrifugation, and stored at 4°C. Supernatants are tested using ELISA kits for IL-1β, IL-6, IL-18, and IL-1α.
Concentrations 40 μM
Incubation time 4 h, 24 h
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 509
Formula C24H33ClN4O6
CAS Number 273404-37-8
Purity 99.68%
Solubility DMSO 90 mg/mL
Storage at -20°C

[1] Hui Yin, et al. Anat Rec (Hoboken). Resibufogenin suppresses growth and metastasis through inducing caspase-1-dependent pyroptosis via ROS-mediated NF-κB suppression in non-small cell lung cancer

[2] Jin-Feng Teng, et al. Cancers (Basel). Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer

[3] Wannamaker W, et al. J Pharmacol Exp Ther. (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.

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Keywords: VX-765 (Belnacasan), Belnacasan supplier, Caspase, inhibitors

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