AS1940477
CAS 928344-12-1 MFCD028344121
化学结构图
SMILES: Cc1ccccc1-n1nc(-c2c(-c3ccc(F)cc3)nn3c2NC[C@@H](CO)C3)ccc1=O
化学属性
| Mol. Weight | 431.46218 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | AS1940477 |
|---|---|
| Formula | C24H22FN5O2 |
| Synonym | AS1940477; AS-1940477; AS 1940477 |
| IUPAC Name | (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 |
| InChIKey | LYHNSWOZRDSWLX-MRXNPFEDSA-N |
| 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 |
| Canonical SMILES | O=C1C=CC(C2=C3NC[C@@H](CO)CN3N=C2C4=CC=C(F)C=C4)=NN1C5=CC=CC=C5C |
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产品应用
- 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 demonst
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