VX 745

Name: VX 745
Brand: Tocris Bioscience
SKU: 3915

Tocris Bioscience a Bio-Techne Brand

Catalog # 3915

Citations (2)

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Key Product Details

Description:	Potent and selective p38α inhibitor
Alternative Names:	VX745, VX-745, Neflamapimod
Chemical Name:	5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one
Purity:	≥98% (HPLC)
Molecular Weight:	436.26

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Biological Activity for VX 745

VX 745 is a highly potent and selective p38α/MAPK14 inhibitor, also inhibits p38β (IC₅₀ values are 10 nM and 220 nM respectively). VX 745 blocks TNFα production in LPS-stimulated HWB in vitro (IC₅₀ = 51-180 nM). Also reduces phosphorylation of p38MAPKα and the downstream target Hsp27, leading to vasodilation, reduces IL-1β levels and amyloid plaques in cortex and hippocampus and lowers CSF tau levels in vivo.

Compound Libraries for VX 745

VX 745 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VX 745 is reviewed on the chemical probes website.

Technical Data for VX 745

M. Wt	436.26
Formula	C₁₉H₉Cl₂F₂N₃OS
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	209410-46-8
PubChem ID	3038525
InChi Key	VEPKQEUBKLEPRA-UHFFFAOYSA-N
Smiles	O=C2N=CN1N=C(SC4=CC=C(F)C=C4F)C=CC1=C2C3=C(Cl)C=CC=C3Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for VX 745

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	43.63	100

Preparing Stock Solutions for VX 745

The following data is based on the product molecular weight 436.26.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.29 mL	11.46 mL	22.92 mL
5 mM	0.46 mL	2.29 mL	4.58 mL
10 mM	0.23 mL	1.15 mL	2.29 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References for VX 745

References are publications that support the biological activity of the product.

Pandey Neflamapimod induces vasodilation in resistance mesenteric arteries by inhibiting p38 MAPKα and downstream Hsp27 phosphorylation. Sci.Rep. 2022 PMID: 35318382
Petrova p38 MAPK signalling regulates cytokine production in IL-33 stimulated type 2 innate lymphoid cells. Sci.Rep. 2020 PMID: 32103032
Alam Selective brain-targeted antagonism of p38 MAPKα reduces hippocampal IL-1 levels and improves Morris Water Maze performance in aged rats. J.Alzheimers Dis. 2015 PMID: 26401942
Duffy The discovery of VX-745: a novel and selective p38α kinase inhibitor. ACS Med.Chem.Lett. 2011 PMID: 24900264
Goldstein Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 2010 PMID: 19950901
Bagley Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg.Med.Chem.Lett. 2007 PMID: 17659871

Citations for VX 745 (2)

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Citations are publications that use Bio-Techne products. Selected citations for VX 745 include:

Singh et al. (2018) Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro. Hum Exp Toxicol. 37:521
PMID: 28629242
Haas et al. (2013) The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells. PLoS Pathog. 9:e1003737
PMID: 24244164

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