Saroglitazar

A PPARα and PPARγ dual agonist

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库存: 现货

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5mg

￥3600.00

2880.00

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10mg

￥5400.00

4320.00

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25mg

￥11875.00

9500.00

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50mg

￥17100.00

13680.00

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100mg

￥24575.00

19660.00

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货号: ajce45000
CAS: 495399-09-2
别名: 沙罗格列扎
分子式: C25H29NO4S
分子量: 439.57
纯度: >98%
溶解度: DMSO : ≥ 25 mg/mL (56.87 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Saroglitazar is a dual agonist of PPARα and PPARγ (EC₅₀s = 0.65 and 3,000 pM, respectively, in a transactivation assay in HepG2 cells).¹ It decreases serum triglyceride, free fatty acid, and glucose levels in a db/db mouse model of diabetes when administered at doses ranging from 0.01 to 3 mg/kg per day for 12 days. It increases insulin sensitivity in an oral glucose challenge when administered at a dose of 1 mg/kg in db/db mice, as well as decreases LDL levels in hApoB100/hCETP mice and in hamsters fed a high-fat high-cholesterol diet. Saroglitazar (10 ?M) reverses palmitic acid-induced decreases in the expression of superoxide dismutase 1 (SOD1), SOD2, glutathione peroxidase (GPX), and catalase and increases in TNF-α, IL-1β, and IL-6 expression in HepG2 cells.² It decreases hepatic inflammation and steatosis in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient high-fat diet when administered at a dose of 3 mg/kg and inhibits fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.

1.Jain, M.R., Giri, S.R., Trivedi, C., et al.Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical modelsPharmacol. Res. Perspect.3(3)e00136(2015) 2.Jain, M.R., Giri, S.R., Bhoi, B., et al.Dual PPARα/γ agonist saroglitazar improves liver histopathology and biochemistry in experimental NASH modelsLiver Int.38(6)1084-1094(2018)

Protocol

Animal experiment:

Rats: Rats randomize based on body weights and are divided into three equal groups and receives the daily administration of vehicle (50% w/v honey for marmoset and 0.1% carboxymethylcellulose for Wistar rats) or Saroglitazar (1.5 and 15 mg/kg per day) for 90 days by oral gavage[1]. Mice: Male C57BL/6J-db/db mice are bled on day 0 to determine pretreatment serum glucose and TG. During next 12 days, each animal is dosed (by oral gavage) with vehicle (0.5% sodium carboxymethyl cellulose) 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, blood samples are collected (1 h after dosing) from orbital sinus under light ether anesthesia. The serum is isolated and analyzed for glucose, TG, free fatty acid (FFA), and insulin levels[1].

参考文献:

[1]. Jain MR, et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136.