A p38α MAPK inhibitor
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VX-745

Item No. 18075

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)thio]-6H-pyrimido[1,6-b]pyridazin-6-one
CAS Number
209410-46-8
Synonyms
  • Neflamapimod
Molecular Formula
C19H9Cl2F2N3OS
Formula Weight
436.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 0.1 mg/ml
λmax
287, 383 nm
SMILES
ClC1=C(C2=C(C=CC(SC3=CC=C(F)C=C3F)=N4)N4C=NC2=O)C(Cl)=CC=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $53

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    10 mg

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    50 mg

    $291

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    Product Description

    VX-745 is an inhibitor of p38α MAPK (IC50 = 9 nM).1 It is selective for p38α over p38β MAPK (Ki = 220 nM) as well as ERK, JNK, and a panel of 50 kinases when used at a concentration of 2 µM. VX-745 inhibits LPS-induced production of IL-1β and TNF-α in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 45 and 51 nM, respectively). It reduces disease severity in a type II collagen-induced mouse model of arthritis when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duffy, J.P., Harrington, E.M., Salituro, F.G., et al. The discovery of VX-745: A novel and selective p38α kinase inhibitor. ACS Med. Chem. Lett. 2(10), 758-763 (2011).