1. GPCR/G Protein Apoptosis
  2. Free Fatty Acid Receptor Apoptosis
  3. DC260126

DC260126 是一种有效的 GPR40 (FFAR1) 拮抗剂。DC260126 剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+ 升高 (IC50 分别 6.28, 5.96, 7.07, 4.58 μM)。DC260126 对棕榈酸酯诱导的内质网应激和凋亡 (apoptosis) 有保护作用。

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DC260126 Chemical Structure

DC260126 Chemical Structure

CAS No. : 346692-04-4

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
In-stock
5 mg ¥500
In-stock
10 mg ¥700
In-stock
25 mg ¥1500
In-stock
50 mg ¥2400
In-stock
100 mg ¥4400
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively)[1]. DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis[2].

体外研究
(In Vitro)

DC260126 reduces GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid in GPR40-CHO cells, suppresses palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulates GPR40 mRNA expression induced by oleic acid in Min6 cells[1].

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

分子量

307.38

Formula

C16H18FNO2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (325.33 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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 3.2533 mL 16.2665 mL 32.5330 mL
5 mM 0.6507 mL 3.2533 mL 6.5066 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.13 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.13 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.74%

参考文献
Animal Administration
[1][2]

Mice[1]
Male C57BL/KsJ-Lepdb (db/db) are maintained in a 12 h light-dark cycle at a temperature of 23°C with free access to water and regular chow diet. To investigate the dose-dependent effect of DC260126, nine-week-old db/db male mice are divided into four groups (n=6/group). Mice are give vehicle (5% DMSO in PBS) or DC260126 (3, 10, 30 mg/kg) once daily by tail vein injection for 5 days. At day 5, each group of mice are fasted for 6 h and blood samples are collected from orbital venous plexus and centrifuged for serum separation. Then the concentration of serum insulin level is measured by ELISA kit. For long term experiments, six-week-old obese db/db male mice are divided into two groups (n=8/group) and given vehicle (5% DMSO in PBS) or DC260126 (10 mg/kg) once daily by tail vein injection for 24 days, respectively.
Rats[2]
Female obese (fa/fa) Zucker rats are maintained in a 12:12 light-dark cycle with free access to water and a high-fat diet containing 15% fat, 1% cholesterol, 0.5% sodium cholate and 15% sucrose, except when fasted before some experiments. Rats at 8 weeks of age are divided into two groups (n=6/group) on the basis of body weight. Rats are injected intraperitoneally once daily with vehicle (propylene glycol) or DC260126 (6 mg/kg) for 8 weeks. Food intake and body weight are monitored periodically. At the end of the experimental period, mice are fasted for 12 h and then blood is collected. Liver, renal, adipose tissues are rapidly excised and weighed. Liver samples are snap frozen in liquid nitrogen and stored at -80°C for western blotting analysis.

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2533 mL 16.2665 mL 32.5330 mL 81.3326 mL
5 mM 0.6507 mL 3.2533 mL 6.5066 mL 16.2665 mL
10 mM 0.3253 mL 1.6267 mL 3.2533 mL 8.1333 mL
15 mM 0.2169 mL 1.0844 mL 2.1689 mL 5.4222 mL
20 mM 0.1627 mL 0.8133 mL 1.6267 mL 4.0666 mL
25 mM 0.1301 mL 0.6507 mL 1.3013 mL 3.2533 mL
30 mM 0.1084 mL 0.5422 mL 1.0844 mL 2.7111 mL
40 mM 0.0813 mL 0.4067 mL 0.8133 mL 2.0333 mL
50 mM 0.0651 mL 0.3253 mL 0.6507 mL 1.6267 mL
60 mM 0.0542 mL 0.2711 mL 0.5422 mL 1.3555 mL
80 mM 0.0407 mL 0.2033 mL 0.4067 mL 1.0167 mL
100 mM 0.0325 mL 0.1627 mL 0.3253 mL 0.8133 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
DC260126
目录号:
HY-101906
需求量: