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MW-150

  Cat. No.:  DC11829   Featured
Chemical Structure
1628502-91-9
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More than 5000 active chemicals with high quality for research!
Field of application
MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM
Chemicals PropertiesBiological activity COAMSDSRelated productsDatasheet
Cas No.: 1628502-91-9
Chemical Name: 6-(4-methylpiperazin-1-yl)-3-(naphthalen-2-yl)-4-(pyridin-4-yl)pyridazine
Synonyms: MW01-18-150SRM;MW 150;MW150
SMILES: C1(C(C2=CC=NC=C2)=CC(N2CCN(C)CC2)=NN=1)C1C=C2C=CC=CC2=CC=1
Formula: C24H23N5
M.Wt: 381.47
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Roy SM, et al. Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models. ACS Chem Neurosci. 2015 Apr 15;6(4):666-80.
Description: MW150 (MW01-18-150SRM) is a selective inhibitor of p38αMAPK isoform with a ki of 101 nM[1].
Target: p38α:101 nM (Ki)
In Vivo: MW150 (2.5 mg/kg; oral daily for 3-4 months) improves the APP/PS1 transgenic (Tg) mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests[1]. MW150 (2.5 mg/kg; given i.p.; daily for 14 days) treatment in APPNLh/NLh × PSP264L/P264L knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT mice[1]. Animal Model: APP/PS1 transgenic (Tg) mouse (overexpresses amyloid-beta)[1] Dosage: 2.5 mg/kg Administration: Oral daily; 3-4 months (until cognitive impairment is present) Result: Improved the Tg mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests.
In Vitro: MW150 inhibits in a concentration-dependent manner the ability of the endogenous p38αMAPK to phosphorylate an endogenous substrate MK2 in activated glia[1]. MW150 blocks in a concentration-dependent manner the increased IL-1β production by activated glia. The IC50 values are 332 nM and 936 nM for MK2 and IL-1β, respectively[1].
References: [1]. Roy SM, et al. Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models. ACS Chem Neurosci. 2015 Apr 15;6(4):666-80.
COA
MSDS
Cat. No. Product name Field of application
DC74349 NuP-3 NuP-3 is a potent, selective MAPK13 and MAPK14 inhibitor with IC50 of 7 and 14 nM, respectively.
DC74347 NC-p38i NC-37 Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.
DC48953 Emprumapimod Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
DC4173 VX-745 VX-745 is a potent and selective inhibitor of p38α MAPK and p38β MAPK with IC50 of 10 nM and 220 nM, respectively.
DC1061 VX-702 (VX702) VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM.
DC8255 SD-06 SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).
DC11829 MW-150 MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM
DC7711 Losmapimod Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
DC10417 Acumapimod (BCT197) Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
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