Fezagepras sodium Setogepram sodium; PBI-4050 sodium|cas:1254472-97-3|西域试剂

Fezagepras sodium Setogepram sodium; PBI-4050 sodium,99.65%

产品编号：Bellancom-100775| CAS NO：1254472-97-3| 分子式：C₁₃H₁₇NaO₂| 分子量：228.26

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货号	价格	库存与货期
Bellancom-100775	￥1800.00	杭州北京（现货）
Bellancom-100775	￥2900.00	杭州北京（现货）
Bellancom-100775	￥9000.00	杭州北京（现货）
Bellancom-100775	￥13500.00	杭州北京（现货）

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Fezagepras sodium Setogepram sodium; PBI-4050 sodium

产品介绍

Fezagepras (Setogepram) sodium 是一种具有口服活性的 GPR40 激动剂和 GPR84 拮抗剂或反向激动剂。Fezagepras sodium 减轻肾，肝和胰腺纤维化。Fezagepras sodium 具有抗纤维化，抗炎和抗增殖作用。

生物活性

Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

体外研究

Fezagepras sodium (500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation.
Fezagepras sodium (250 or 500 µM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	HSCs
Concentration:	250 or 500 µM
Incubation Time:	24 hours
Result:	Inhibited TGF-β-activated HSC proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%.

Cell Cycle Analysis

Cell Line:	HSCs
Concentration:	250 µM, 500 µM
Incubation Time:	24 hours
Result:	Inhibited cell cycle progression.

体内研究
(In Vivo)

Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS^-/-db/db mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Type 2 diabetes eNOS^-/-db/db mice
Dosage:	100 mg/kg/day
Administration:	Given via daily gavage from 8-20 weeks
Result:	Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved.

体内研究

Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS^-/-db/db mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Type 2 diabetes eNOS^-/-db/db mice
Dosage:	100 mg/kg/day
Administration:	Given via daily gavage from 8-20 weeks
Result:	Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved.

体内研究

Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS^-/-db/db mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Type 2 diabetes eNOS^-/-db/db mice
Dosage:	100 mg/kg/day
Administration:	Given via daily gavage from 8-20 weeks
Result:	Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved.

性状

Solid

溶解性数据

In Vitro:

H₂O : ≥ 100 mg/mL (438.10 mM)

DMSO : ≥ 64 mg/mL (280.38 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3810 mL	21.9048 mL	43.8097 mL
5 mM	0.8762 mL	4.3810 mL	8.7619 mL
10 mM	0.4381 mL	2.1905 mL	4.3810 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 120 mg/mL (525.72 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。