Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fezagepras sodium (Setogepram sodium salt) 是口服有效的 GPR40 激动剂及 GPR84 拮抗剂或反向激动剂。Fezagepras sodium 可以减轻肝,肾和胰腺纤维化。Fezagepras sodium 具有抗炎,抗增殖和抗纤维化作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 622 | 现货 | ||
5 mg | ¥ 1,450 | 现货 | ||
10 mg | ¥ 2,360 | 现货 | ||
25 mg | ¥ 3,920 | 现货 | ||
50 mg | ¥ 5,720 | 现货 | ||
100 mg | ¥ 7,960 | 现货 | ||
500 mg | ¥ 15,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,590 | 现货 |
产品描述 | Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions. |
体外活性 | PBI-4050 inhibited kidney macrophage infiltration, oxidative stress, and TGF-β-mediated fibrotic signaling pathways, and it also protected against the development of tubulointerstitial fibrosis. To confirm a direct antiinflammatory/antifibrotic effect in the kidney, further studies with a nondiabetic model of EGFR-mediated proximal tubule activation confirmed that PBI-4050 dramatically decreased the development of the associated tubulointerstitial injury and macrophage infiltration[1]. |
体内活性 | eNOS-/- db/db mice were treated with PBI-4050 from 8-20 weeks of age (early treatment) or from 16-24 weeks of age (late treatment). PBI-4050 treatment ameliorated the fasting hyperglycemia and abnormal glucose tolerance tests seen in vehicle-treated mice. In addition, PBI-4050 preserved (early treatment) or restored (late treatment) blood insulin levels and increased autophagy in islets. PBI-4050 treatment led to significant improvements in lifespan in the diabetic mice. Both early and late PBI-4050 treatment protected against progression of DN, as indicated by reduced histological glomerular injury and albuminuria, slow decline of glomerular filtration rate, and loss of podocytes[1]. |
别名 | Setogepram sodium salt, PBI-4050 sodium salt |
分子量 | 228.26 |
分子式 | C13H17NaO2 |
CAS No. | 1254472-97-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 90.0 mg/mL (394.3 mM)
DMSO: 57.6 mg/mL (252.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 4.381 mL | 21.9048 mL | 43.8097 mL | 109.5242 mL |
5 mM | 0.8762 mL | 4.381 mL | 8.7619 mL | 21.9048 mL | |
10 mM | 0.4381 mL | 2.1905 mL | 4.381 mL | 10.9524 mL | |
20 mM | 0.219 mL | 1.0952 mL | 2.1905 mL | 5.4762 mL | |
50 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1905 mL | |
100 mM | 0.0438 mL | 0.219 mL | 0.4381 mL | 1.0952 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Fezagepras sodium 1254472-97-3 Endocrinology/Hormones GPCR/G Protein GPR Setogepram sodium Setogepram sodium salt PBI-4050 sodium PBI-4050 sodium salt Inhibitor inhibitor inhibit