沙羅格列扎鎂鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetSaroglitazar MagnesiumCat. No.: HY-19937ACAS No.: 1639792-20-3分式: CHMgNOS分量: 901.42作靶點: PPAR作通路: Cell Cycle/DNA Damage儲存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 month (sealed storage, away frommoisture)溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (55.47 mM; Need

2、 ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.1094 mL 5.5468 mL 11.0936 mL5 mM 0.2219 mL 1.1094 mL 2.2187 mL10 mM 0.1109 mL 0.5547 mL 1.1094 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 (sealed storage, a

3、way from moisture)。-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?。以下溶解案都請先按?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: 2

4、.75 mg/mL (3.05 mM); Clear solution此案可獲得 2.75 mg/mL (3.05 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 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: 2.75 mg/mL (3.05 mM); Suspended solution; Need ultra

5、sonic此案可獲得 2.75 mg/mL (3.05 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (3.05 mM); Clear solution此案可獲得 2.75 mg/mL (3.05 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

6、例，取 100 L 27.5 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Saroglitazar magnesium 種新型的過氧化物酶體增殖物活化受體PPAR的激動劑，具有顯著PPAR活性和中度PPAR 活性，在HepG2細(xì)胞中的EC50值分別為0.65 pM and 3 nM。IC & Target PPAR PPAR0.65 pM (EC50, HepG2 3 nM (EC50, HepG2 cell)cell)體內(nèi)研究 In db/db mice, 12-day treatment with Saroglitaza

7、r (0.01-3 mg/kg per day, orally) causes dose-dependent reductionsin serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral

8、glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats andmarmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associatedside effects in humans. Based on efficacy and safety profile, Saroglitazar appears

9、 to have good potential as noveltherapeutic agent for treatment of dyslipidemia and diabetes1.PROTOCOLAnimal Rats: Rats randomize based on body weights and are divided into three equal groups and receives the dailyAdministration 1 administration of vehicle (50% w/v honey for marmoset and 0.1% carbox

10、ymethylcellulose for Wistar rats) orSaroglitazar (1.5 and 15 mg/kg per day) for 90 days by oral gavage1.Mice: Male C57BL/6J-db/db mice are bled on day 0 to determine pretreatment serum glucose and TG. During next 12days, each animal is dosed (by oral gavage) with vehicle (0.5% sodium carboxymethyl c

11、ellulose) or Saroglitazar (0.01,0.03, 0.1, 0.3,1, and 3 mg/kg per day) or pioglitazone (60 mg/kg per day) and on day 12 of the treatment, bloodsamples are collected (1 h after dosing) from orbital sinus under light ether anesthesia. The serum is isolated andanalyzed for glucose, TG, free fatty acid

12、(FFA), and insulin levels1.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) Patent. US20190388398A1.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCESPage 2 of 3 www.MedChemE1. Jain MR, et al. Saroglitazar, a novel PPAR/ agonist with predominant PPAR activity, shows lipid-lowering and insulin-sensitizing effects in preclinicalmodels. Pharmacol Res Perspect. 2015 Jun;3(3):e00136.McePdfHeightCaution: Product has