VX 745
Tocris Bioscience, part of Bio-Techne | Catalog # 3915
Potent and selective p38α inhibitor
Key Product Details
Description
Potent and selective p38α inhibitor
Alternative Names
VX745,VX-745,Neflamapimod
Product Description
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.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.Product Specifications
Molecular Weight
436.26
Formula
C19H9Cl2F2N3OS
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
5-(2,6-Dichlorophenyl)-2-[2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- 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
- Petrova p38 MAPK signalling regulates cytokine production in IL-33 stimulated type 2 innate lymphoid cells. Sci.Rep. 2020 PMID: 32103032
- Pandey Neflamapimod induces vasodilation in resistance mesenteric arteries by inhibiting p38 MAPKα and downstream Hsp27 phosphorylation. Sci.Rep. 2022 PMID: 35318382
- 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
Product Specific Notices for VX 745
For research use only
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