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AS1940477

NMR下載 COA and HPLC MSDS下載
names：
(R)-6-(2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl)-2-(o-tolyl)pyridazin-3(2H)-one
CAS號：
928344-12-1
MDL Number：
MF(分子式)： C24H22FN5O2 MW(分子量)： 431.46218
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	AS1940477
英文別名	AS1940477; AS-1940477; AS 1940477
CAS號	928344-12-1
Inchi	InChI=1S/C24H22FN5O2/c1-15-4-2-3-5-20(15)30-21(32)11-10-19(27-30)22-23(17-6-8-18(25)9-7-17)28-29-13-16(14-31)12-26-24(22)29/h2-11,16,26,31H,12-14H2,1H3/t16-/m1/s1
InchiKey	LYHNSWOZRDSWLX-MRXNPFEDSA-N
分子式 Formula	C24H22FN5O2
分子量 Molecular Weight	431.46218
溶解度Solubility
性狀	white solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	AS1940477(CAS:928344-12-1):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg/kg (ED(50)=0.053 mg/kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this study demonstrated that AS1940477 is a novel and potent p38 MAPK inhibitor and may be useful as a promising anti-inflammatory agent for treating inflammatory disorders.
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[1]Terajima M, Inoue T, Magari K, Yamazaki H, Higashi Y, Mizuhara H. Anti-inflammatory effect and selectivity profile of AS1940477, a novel and potent p38 mitogen-activated protein kinase inhibitor. Eur J Pharmacol. 2013 Jan 5;698(1-3):455-62. doi: 10.1016/j.ejphar.2012.11.02[1]Epub 2012 Nov 23. PubMed PMID: 23183108.

[2]Asano T, Yamazaki H, Kasahara C, Kubota H, Kontani T, Harayama Y, Ohno K, Mizuhara H, Yokomoto M, Misumi K, Kinoshita T, Ohta M, Takeuchi M. Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyr imidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. J Med Chem. 2012 Sep 13;55(17):7772-85. doi: 10.1021/jm3008008. Epub 2012 Aug 31. PubMed PMID: 22905713.

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