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  3. L-168049

L-168049 是一种有效的、选择性的、具有口服活性的非竞争性胰高血糖素受体 (glucagon receptor) 拮抗剂,对人、鼠和犬胰高血糖素受体的 IC50 分别为 3.7 nM,63 nM 和 60 nM。

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L-168049 Chemical Structure

L-168049 Chemical Structure

CAS No. : 191034-25-0

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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 ¥2475
In-stock
1 mg ¥1022
In-stock
5 mg ¥2250
In-stock
10 mg ¥3500
In-stock
25 mg ¥7000
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively[1][2].

IC50 & Target

IC50: 3.7 nM (human glucagon receptor), 63 nM (murine glucagon receptor), and 60 nM (canine glucagon receptor)[2]

体外研究
(In Vitro)

L-168049 (compound 49) inhibits glucagon (100 pM) stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor (hGIAR) (IC50 of 41 nM). L-168049 blocks cAMP formation stimulated by glucagon in murine liver membranes[1].
L-168049 increases the apparent EC50 for glucagon stimulation of adenylyl cyclase in Chinese hamster ovary cells expressing the human glucagon receptor and decreases the maximal glucagon stimulation observed, with a Kb of 25 nM[2].

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

体内研究
(In Vivo)

In the liver of L-G6pc−/- mice, Pck1 mRNA expression is decreased by half 6 h after the administration of L-168049 (50 mg/kg body; p.o.), demonstrating the efficiency of the suppression of glucagon signaling. In agreement with the role of glucagon in the induction of extrahepatic gluconeogenesis, the administration of the L-168049 prevents the increase of the G6pc expression in both the kidneys and intestine of 6 h-fasted L-G6pc−/- mice[3].

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

分子量

467.79

Formula

C24H20BrClN2O

CAS 号
性状

固体

颜色

Light yellow to yellow

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 50 mg/mL (106.89 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 2.1377 mL 10.6886 mL 21.3771 mL
5 mM 0.4275 mL 2.1377 mL 4.2754 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, 6 months; -20°C, 1 month。-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。

  • 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

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

L-168049 相关分类

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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1377 mL 10.6886 mL 21.3771 mL 53.4428 mL
5 mM 0.4275 mL 2.1377 mL 4.2754 mL 10.6886 mL
10 mM 0.2138 mL 1.0689 mL 2.1377 mL 5.3443 mL
15 mM 0.1425 mL 0.7126 mL 1.4251 mL 3.5629 mL
20 mM 0.1069 mL 0.5344 mL 1.0689 mL 2.6721 mL
25 mM 0.0855 mL 0.4275 mL 0.8551 mL 2.1377 mL
30 mM 0.0713 mL 0.3563 mL 0.7126 mL 1.7814 mL
40 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3361 mL
50 mM 0.0428 mL 0.2138 mL 0.4275 mL 1.0689 mL
60 mM 0.0356 mL 0.1781 mL 0.3563 mL 0.8907 mL
80 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.6680 mL
100 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5344 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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Inquiry Information

产品名称:
L-168049
目录号:
HY-103547
需求量: