洛批莫德作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetLosmapimodCat. No.: HY-10402CAS No.: 585543-15-3分式: CHFNO分量: 383.46作靶點: p38 MAPK; Autophagy作通路: MAPK/ERK Pathway; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 58 mg/mL (151.25 mM)* means soluble, but saturation unknown.SolventMass1

2、 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付?/p>

3、請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.77 mg/mL (2.01 mM); Clear solution此案可獲得 0.77 mg/mL (2.01 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取

4、 100 L 7.7 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.77 mg/mL (2.01 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 0.77 mg/mL (2.01 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 7.7 mg/mL 的澄 DMSO 儲備液

5、加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.77 mg/mL (2.01 mM); Clear solution此案可獲得 0.77 mg/mL (2.01 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 7.7 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Losmapimod種有效，選擇性，可服的 p38 MAPK 抑制劑，抑制p38 和 p3

6、8 的 pKi 值分別為 8.1 和 7.6。IC & Target pKi: 8.1 (p38), 7.6 (p38)體內(nèi)研究 In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly anddose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices ofrenal function,

7、 and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA),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): normalAdministration 1 diet controls (ND), high s

8、alt-fat diet controls (SFD), SFD + GSK-AHAB (1.2 mg/kg/day), and SFD + GSK-AHAB (12mg/kg/day) and SFD + MK 966 (18 mg/kg/day). All drugs are administered in the diet by mixing with the SFD. Asubgroup of animals from each group (n=6 per group) are anesthetized and surgically instrumented withradiotel

9、emetry units for the conscious measurement of mean arterial blood pressure and heart rate. These animalsare allowed to recover for at least 7 days before the start of the study.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Syst. 2018

10、Apr 25;6(4):424-443.e7. EBioMedicine. 2018 Feb;28:51-61. Am J Physiol Lung Cell 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.MedChemE www.MedChemEREFERENCES1. Willette RN, et al. Differential effects

11、of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. JPharmacol Exp Ther. 2009 Sep;330(3):964-70.Page 2 of 3 www.MedChemE2. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38 MAPK inhibition.Neurochem Int. 2015 Nov;90:1-8.McePdfHeightCaution: Product has not been fully valida