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VX-745 - ≥98%, high purity , MAP kinase p38 alpha inhibitor, CAS No.209410-46-8, MAP kinase p38 alpha inhibitor

  • Moligand™
  • ≥98%
Item Number
V126681
Grouped product items
SKUSizeAvailabilityPrice Qty
V126681-10mg
10mg
In stock
$86.90
V126681-25mg
25mg
In stock
$195.90
V126681-50mg
50mg
In stock
$260.90
V126681-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$469.90
V126681-250mg
250mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$1,057.90

Potent, selective p38 alpha MAPK inhibitor

Basic Description

Synonyms209410-46-8|VX-745|Neflamapimod|5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido[1,6-b]pyridazin-6-one|VX 745|VX745|5-(2,6-dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyrimido[1,6-b]pyridazin-6-one|C19H9Cl2F2N3OS|VRT-031745|Neflamapimod [
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsVX-745 is highly potent and selective p38α inhibitor (IC50 = 10 nM). VX-745 also blocks TNFα production in LPS-stimulated HWB in vitro (IC50 = 177 nM). VX-745 displays 1000-fold selectivity over closely related kinases, including ERK1, MK2 and
Storage TempProtected from light,Store at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionMAP kinase p38 alpha inhibitor
NoteNeed more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Product Properties

ALogP5.1

Names and Identifiers

IUPAC Name 5-(2,6-dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyrimido[1,6-b]pyridazin-6-one
INCHI InChI=1S/C19H9Cl2F2N3OS/c20-11-2-1-3-12(21)17(11)18-14-5-7-16(25-26(14)9-24-19(18)27)28-15-6-4-10(22)8-13(15)23/h1-9H
InChi Key VEPKQEUBKLEPRA-UHFFFAOYSA-N
Canonical SMILES C1=CC(=C(C(=C1)Cl)C2=C3C=CC(=NN3C=NC2=O)SC4=C(C=C(C=C4)F)F)Cl
Isomeric SMILES C1=CC(=C(C(=C1)Cl)C2=C3C=CC(=NN3C=NC2=O)SC4=C(C=C(C=C4)F)F)Cl
PubChem CID 3038525
Molecular Weight 436.27

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
L2123153Certificate of AnalysisOct 08, 2023 V126681
L2123154Certificate of AnalysisOct 08, 2023 V126681
L2123399Certificate of AnalysisOct 08, 2023 V126681
L2123421Certificate of AnalysisOct 08, 2023 V126681
L2123430Certificate of AnalysisOct 08, 2023 V126681

Chemical and Physical Properties

SolubilityDMSO ≥60mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL;Chloroform, DMSO, Methanol
Sensitivitylight sensitive
Melt Point(°C)259-262°C (dec.)

Related Documents

References

1. Fitzgerald CE, Patel SB, Becker JW, Cameron PM, Zaller D, Pikounis VB, O'Keefe SJ, Scapin G.  (2003)  Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity..  Nat Struct Biol,  10  (9): (764-9).  [PMID:12897767]
2. Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT et al..  (2008)  A quantitative analysis of kinase inhibitor selectivity..  Nat Biotechnol,  26  (1): (127-32).  [PMID:18183025]
3. Munoz L, Ralay Ranaivo H, Roy SM, Hu W, Craft JM, McNamara LK, Chico LW, Van Eldik LJ, Watterson DM.  (2007)  A novel p38 alpha MAPK inhibitor suppresses brain proinflammatory cytokine up-regulation and attenuates synaptic dysfunction and behavioral deficits in an Alzheimer's disease mouse model..  J Neuroinflammation,  (3): (21).  [PMID:17784957]
4. Duffy JP, Harrington EM, Salituro FG, Cochran JE, Green J, Gao H, Bemis GW, Evindar G, Galullo VP, Ford PJ et al..  (2011)  The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor..  ACS Med Chem Lett,  (10): (758-63).  [PMID:24900264]
5. Alam JJ.  (2015)  Selective Brain-Targeted Antagonism of p38 MAPKα Reduces Hippocampal IL-1β Levels and Improves Morris Water Maze Performance in Aged Rats..  J Alzheimers Dis,  48  (1): (219-27).  [PMID:26401942]
6. Alam J, Blackburn K, Patrick D.  (2017)  Neflamapimod: Clinical Phase 2b-Ready Oral Small Molecule Inhibitor of p38α to Reverse Synaptic Dysfunction in Early Alzheimer's Disease..  J Prev Alzheimers Dis,  (4): (273-278).  [PMID:29181493]

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