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CAS No.: 585543-15-3

Losmapimod/洛批莫德 Catalog No. CSN18346

Synonyms: GSK-AHAB;GW856553X;SB856553

Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 p38 MAPKβ

pKi:7.6 p38 MAPKα

pKi:8.1
描述Mitogen-activated protein kinase p38 is a stress-induced intracellular kinase that plays essential roles in the regulation of cellular responses, including migration, cytokine expression, and contraction. Losmapimod is a potent, orally active inhibitor of p38α and p38β with pK_i values of 8.1 and 7.6, respectively^[1]. In gefitinib-resistant cells (HCC827GR and H1975), treatment of 1 μM losmapimod for 10 hours inhibited gefitinib-induced phosphorylation of STAT3 and expressions of p21 and cyclin D1. Combined treatment of gefitinib (1 μM) and losmapimod (1 μM) significantly suppressed anchorage-independent cell growth and proliferation in NSCLC cells^[2]. Spontaneously hypertensive stroke-prone rat (SHR-SP) placed on high salt-fat diet (SFD) for 8 weeks showed 50% survival rate and increased mean blood pressure. Dietary administration of losmapimod (1.2 and 12 mg/kg/day doses) significantly elevated the survival rate. Animals receiving 12 mg/kg/day losmapimod also showed suppressed mean blood pressure compared to untreated SFD-fed rats. Treatment of losmapimod (1.2 and 12 mg/kg/day doses) for 6 weeks attenuated SFD-induced increase in urine flow, FENa, albumin excretion, creatinine clearance, and kidney weight. Rats administered with 12 mg/kg/day losmapimod showed reduced left ventricular mass and wall thickness compared with untreated SFD-fed rats. Endothelial-dependent and endothelium-independent vasorelaxation were also improved by losmapimod treatment at a dose-dependent manner^[1].
作用机制Losmapimod selectively and potently inhibits p38 via competing for the kinase ATP binding site^[1].
动物研究
剂量
Mice: 12 mg/kg^[2] (p.o.) Rat: 1.8 mg/kg^[3] (i.p.)

给药途径
p.o., i.p.
临床研究

动物研究
剂量	Mice: 12 mg/kg^[2] (p.o.) Rat: 1.8 mg/kg^[3] (i.p.)
给药途径	p.o., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01648192	Acute Coronary Syndrome	Phase 1	Completed	-	Australia, New South Wales ... more >> GSK Investigational Site Randwick, New South Wales, Australia, 2031 Collapse <<
NCT00633022	Atherosclerosis	Phase 2	Completed	-	United Kingdom ... more >> GSK Investigational Site Oxford, Oxfordshire, United Kingdom, OX3 9DU GSK Investigational Site Cambridge, United Kingdom, CB2 2GG GSK Investigational Site London, United Kingdom, E1 1B3 GSK Investigational Site London, United Kingdom, Se1 7EH Collapse <<
NCT01039961	Cardiovascular Disease	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Cambridge, United Kingdom, CB2 2GG Collapse <<

更多
参考文献

[1] Willette RN, Eybye ME, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70.
[2] Yeung YT, Yin S, et al. Losmapimod Overcomes Gefitinib Resistance in Non-small Cell Lung Cancer by Preventing Tetraploidization. EBioMedicine. 2018.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6078 mL
- 13.0392 mL
- 26.0783 mL
- 5 mM
- 0.5216 mL
- 2.6078 mL
- 5.2157 mL
- 10 mM
- 0.2608 mL
- 1.3039 mL
- 2.6078 mL

技术信息

CAS号

585543-15-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H26FN3O2

运输

蓝冰

分子量

383.46

别名

GSK-AHAB;GW856553X;SB856553;GW-856553;洛批莫德

溶解度

DMSO	330.0 mg/mL (860.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	6 mg/mL	clear
PO	0.5% CMC-Na	40 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01648192	Acute Coronary Syndrome	Phase 1	Completed	-	Australia, New South Wales ... more >> GSK Investigational Site Randwick, New South Wales, Australia, 2031 Collapse <<
NCT00633022	Atherosclerosis	Phase 2	Completed	-	United Kingdom ... more >> GSK Investigational Site Oxford, Oxfordshire, United Kingdom, OX3 9DU GSK Investigational Site Cambridge, United Kingdom, CB2 2GG GSK Investigational Site London, United Kingdom, E1 1B3 GSK Investigational Site London, United Kingdom, Se1 7EH Collapse <<
NCT01039961	Cardiovascular Disease	Phase 1	Completed	-	United Kingdom ... more >> GSK Investigational Site Cambridge, United Kingdom, CB2 2GG Collapse <<
NCT00633022	-	-	Completed	-	-
NCT01218126	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	-
NCT02145468	Acute Coronary Syndrome	Phase 3	Completed	-	-
NCT01756495	Acute Coronary Syndrome	Phase 1	Completed	-	United States, Maryland ... more >> GSK Investigational Site Baltimore, Maryland, United States, 21225 Collapse <<
NCT02000440	Glomerulosclerosis, Focal Segm... more >>ental Collapse <<	Phase 2	Completed	-	United States, California ... more >> GSK Investigational Site Los Angeles, California, United States, 90025 GSK Investigational Site Stanford, California, United States, 94304 United States, Louisiana GSK Investigational Site New Orleans, Louisiana, United States, 70112 United States, Michigan GSK Investigational Site Ann Arbor, Michigan, United States, 48109 United States, North Carolina GSK Investigational Site Chapel Hill, North Carolina, United States, 27599-7155 United States, Ohio GSK Investigational Site Cleveland, Ohio, United States, 44109 GSK Investigational Site Columbus, Ohio, United States, 43210 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19140 Canada, Alberta GSK Investigational Site Edmonton, Alberta, Canada, T6G 2B7 Canada, British Columbia GSK Investigational Site Vancouver, British Columbia, Canada, V6Z 1Y6 Canada, Ontario GSK Investigational Site Toronto, Ontario, Canada, M4N 3M5 GSK Investigational Site Toronto, Ontario, Canada, M5G 2C4 Collapse <<
NCT01218126	-	-	Completed	-	-
NCT02299375	-	-	Completed	-	-
NCT02299375	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	-
NCT02000440	-	-	Completed	-	-
NCT02145468	-	-	Completed	-	-
NCT01541852	Chronic Obstructive Pulmonary ... more >>Disease Collapse <<	Phase 2	Completed	-	United Kingdom ... more >> Cambridge University Hospitals NHS Foundation Trust Cambridge, Cambridgeshire, United Kingdom, CB2 0QQ Royal Brompton & Harefield NHS Foundation Trust London, United Kingdom, SW3 6NP Collapse <<

靶点	Description	IC50
p38 MAPKβ		pKi:7.6
p38 MAPKα		pKi:8.1

Losmapimod/洛批莫德 Catalog No. CSN18346

靶点选择性

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