Belnacasan

SKU: orb1301082

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Description

Belnacasan

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience

Images & Validation

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Key Properties

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CAS Number	273404-37-8
MW	509.0
Purity	>98%
Formula	C₂₄H₃₃ClN₄O₆
SMILES	CCO[C@@H]1OC(=O)C[C@@H]1NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)c1ccc(N)c(Cl)c1)C(C)(C)C
Target	Protease
Solubility	Soluble in DMSO (up to 25 mg/ml)

Bioactivity

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Target IC50	Caspase-4:< 0.6 nM (Ki)\|Caspase-1:0.8 nM (Ki)
In Vivo	VRT-043198 inhibits the release of IL-1β from peripheral blood mononuclear cells (PBMCs) and whole blood, with IC50 values of 0.67 μM and 1.9 μM, respectively. VX-765, an orally bioavailable prodrug of VRT-043198, demonstrates potent inhibition of ICE/caspase-1 and caspase-4, with Ki values of 0.8 nM and <0.6 nM, respectively. Read more...
In Vitro	VX-765 demonstrates antiepileptic properties by preventing the increase of IL-1β in the forebrain astrocytes of rats, thereby inhibiting the occurrence of epilepsy without significantly affecting the duration of post-discharge. In adult rats with genetic absence epilepsy, a 3-day administration of VX-765 significantly reduces the cumulative duration and decreases the average spike-wave discharges by 55% through the selective blockade of IL-1β biosynthesis. In acute epileptic mouse models, doses ranging from 50 mg/kg to 200 mg/kg of VX-765 delay the onset of the first epileptic episode and reduce the average number of seizures by 50% and the total duration by 64%. Additionally, a 200 mg/kg dose in a collagen-induced arthritis mouse model suppresses 60% of lipopolysaccharide-induced IL-1β production and leads to a dose-dependent significant reduction in inflammation scores, effectively protecting against joint lesions. Read more...
Cell Research	VX-765 is solubilized in DMSO and stored, and then diluted with RPMI 1640 complete medium (DMSO 0.2%) before use. 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 VX-765 (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. Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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VX-765

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Compound Identifiers

PubChem CID

11398092 ↗

Key Properties

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No computed properties available.

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Belnacasan (orb1301082)

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CAS Number:	244133-31-1
MW:	480.94
Formula:	C₂₂H₂₉ClN₄O₆

Purity:	>98% (HPLC)
CAS Number:	273404-37-8
MW:	508.995
Formula:	C₂₄H₃₃ClN₄O₆

Belnacasan

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

VRT-043198 [orb1739848]

VX-765 [orb1225453]

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Belnacasan (orb1301082)

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