VX-765 (Belnacasan)

Catalog No. A10984

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。

Product Citations

Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054

Technical details

Catalog Num	A10984
M. Wt	509.0
Formula	C24H33ClN4O6
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	273404-37-8
Synonyms	VX765
SMILES	CCO[C@H]1[C@H](CC(=O)O1)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C(C)(C)C)NC(=O)C3=CC(=C(C=C3)N)Cl

Biological Activity

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。

Targets

Caspase-4 (Cell-free assay)	Caspase-1 (Cell-free assay)
<0.6 nM(Ki)	0.8 nM(Ki)

Solubility *

In vitro (25°C)	DMSO	Warmed: 87 mg/mL (170.92 mM)
	Water	Insoluble
	Ethanol	Warmed: 87 mg/mL (170.92 mM)
In vivo	2% DMSO+30% PEG 300+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.65 mL	98.23 mL	196.46 mL
0.5 mM	3.93 mL	19.65 mL	39.29 mL
1 mM	1.96 mL	9.82 mL	19.65 mL
5 mM	0.39 mL	1.96 mL	3.93 mL

*The above data is based on the productmolecular weight 509.0 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.