| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S88723-2mg | 98% | ￥475.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S88723-5mg | 98% | ￥740.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S88723-10mg | 98% | ￥1230.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S88723-25mg | 98% | ￥2350.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S88723-50mg | 98% | ￥3900.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S88723-100mg | 98% | ￥5700.00元 | 预计交期：2-3天 | - | - | - |
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| 产品描述： Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist | ||||||||||||||||||||
| 靶点： PPAR-δ:2 nM (EC50);PPAR-α:1600 nM (EC50);PPAR | ||||||||||||||||||||
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体外研究： Seladelpar (MBX-8025) is an orally active, potent (2 nM), and specific (>750-fold and >2500-fold compared with PPAR-α or PPAR-γ receptors, respectively) PPAR-δ agonist being developed as a lipid-altering agent. Seladelpar is a potent, and selective PPAR-δ agonist (50% effect concentration human PPAR-δ=2 nM, PPAR-α=1,600 nM) that demonstrates favorable effects on insulin resistance, diabetes, and atherogenic dyslipidemia |
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体内研究： From weaning, female Alms1 mutant (foz/foz) mice and wild-type littermates are fed an atherogenic diet for 16 weeks; groups (n=8-12) are then randomized to receive Seladelpar (10 mg/kg) or vehicle (1% methylcellulose) by gavage for 8 weeks. Despite minimally altering body weight, Seladelpar normalizes hyperglycemia, hyperinsulinemia, and glucose disposal in foz/foz mice. Serum alanine aminotransferase ranges 300-600 U/L in vehicle-treated foz/foz mice; Seladelpar reduces alanine aminotransferase by 50%. In addition, Seladelpar normalizes serum lipids and hepatic levels of free cholesterol and other lipotoxic lipids that are increased in vehicle-treated foz/foz versus wild-type mice. This abolished hepatocyte ballooning and apoptosis, substantially reduce steatosis and liver inflammation, and improve liver fibrosis. In vehicle-treated foz/foz mice, the mean nonalcoholic fatty liver disease activity score is 6.9, indicating nonalcoholic steatohepatitis (NASH); Seladelpar reverses NASH in all foz/foz mice (nonalcoholic fatty liver disease activity score 3.13). In atherogenic diet-fed Wt mice, administration of Seladelpar reduces body weight by ∼18% (P<0.05). In contrast, Seladelpar produces minimal effect on body weight in atherogenic diet–fed foz/foz mice. These animals develope severe hyperglycemia, hyperinsulinemia, and whole-body insulin resistance after 16 weeks (P<0.05); Seladelpar strikingly improves these indices (P<0.05). After intraperitoneal glucose injection, blood glucose reaches ~32 mM in |
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参考文献： 1. Bays HE, et al. MBX-8025, a novel peroxisome proliferator receptor-delta agonist: lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J Clin Endocrinol Metab. 2011 Sep;96(9):2889-97. 2. Haczeyni F, et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol Commun. 2017 Jul 31;1(7):663-674. |
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| 溶解性： Soluble in DMSO | ||||||||||||||||||||
| 保存条件： -20°C | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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