貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S88723-2mg	≥98%	￥475.00 S88723-2mg ￥475.00 2-3天	0 貨期：2-3天	-	-	-
S88723-5mg	≥98%	￥740.00 S88723-5mg ￥740.00 2-3天	0 貨期：2-3天	-	-	-
S88723-10mg	≥98%	￥1230.00 S88723-10mg ￥1230.00 2-3天	0 貨期：2-3天	-	-	-
S88723-25mg	≥98%	￥2350.00 S88723-25mg ￥2350.00 2-3天	0 貨期：2-3天	-	-	-
S88723-50mg	≥98%	￥3900.00 S88723-50mg ￥3900.00 2-3天	0 貨期：2-3天	-	-	-
S88723-100mg	≥98%	￥5700.00 S88723-100mg ￥5700.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist

產(chǎn)品描述：

Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist

靶點(diǎn)：

PPAR-δ:2 nM (EC50);PPAR-α:1600 nM (EC50);PPAR

體外研究：

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

體內(nèi)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

參考文獻(xiàn)：

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.

溶解性：

Soluble in DMSO

保存條件：

-20°C

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.25 ml	11.249 ml	22.499 ml
5 mM	0.45 ml	2.25 ml	4.5 ml
10 mM	0.225 ml	1.125 ml	2.25 ml
50 mM	0.045 ml	0.225 ml	0.45 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

質(zhì)檢證書(COA)

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批號(hào)：JS298415 貨號(hào)：S20001-25g
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MBX 8025

Seladelpar