Losmapimod-GSK-AHAB-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELosmapimodCat. No.: HY-10402CAS No.: 585543-15-3Synonyms: GSK-AHAB; GW856553X; SB856553分式: CHFNO分量: 383.46作靶点: p38 MAPK; Autophagy作通路: MAPK/ERK Pathway; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性数据体外实验 DMSO : 58 mg/mL (151.25 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6078 mL 13.0392 mL 26.0783 mL5 mM 0.5216 mL 2.6078 mL 5.2157 mL10 mM 0.2608 mL 1.3039 mL 2.6078 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解

3、案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.77 mg/mL (2.01 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.77 mg/mL (2.01 mM); Clear solu

4、tion1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.77 mg/mL (2.01 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Losmapimod种有效，选择性，可服的 p38 MAPK 抑制剂，抑制p38 和 p38 的 pKi 值分别为 8.1 和7.6。IC50 & Target pKi: 8.1 (p38), 7.6 (p38)体内研究 In the spontaneously hypertens

5、ive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHABsignificantly and dose-dependently improves survival, endothelial-dependent and -independent vascularrelaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling,plasma renin activity (PRA),

6、aldosterone, and interleukin-1 (IL-1) 1.PROTOCOLAnimal Male SHR-SPs (n=70) are randomly assigned according to body weight into five groups (n=14 per group):Administration 1 normal diet controls (ND), high salt-fat diet controls (SFD), SFD + GSK-AHAB (1.2 mg/kg/day), and SFD +GSK-AHAB (12 mg/kg/day)

7、and SFD + rofecoxib (18 mg/kg/day). All drugs are administered in the diet bymixing with the SFD. A subgroup of animals from each group (n=6 per group) are anesthetized withisoflurane and surgically instrumented with radiotelemetry units for the conscious measurement of meanarterial blood pressure a

8、nd heart rate. These animals are allowed to recover for at least 7 days before thestart of the study.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Syst. 2018 Apr 25;6(4):424-443.e7. EBioMedicine. 2018 Feb;28:51-61. Am J Physiol Lung C

9、ell Mol Physiol. 2012 Nov 15;303(10):L929-38. Neurochem Int. 2015 Nov;90:1-8. Patent. US20180296546A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Willette RN, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model ofca

10、rdiovascular disease. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70.2. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38MAPK inhibition. Neurochem Int. 2015 Nov;90:1-8.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: Product has not been fully vali