L-798106 CM9; GW671021,99.85%

产品编号:Bellancom-15274| CAS NO:244101-02-8| 分子式:C27H22BrNO4S| 分子量:536.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-15274
1560.00 杭州 北京(现货)
Bellancom-15274
2496.00 杭州 北京(现货)
Bellancom-15274
5460.00 杭州 北京(现货)
Bellancom-15274
8775.00 杭州 北京(现货)
Bellancom-15274
14040.00 杭州 北京(现货)

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L-798106 CM9; GW671021

产品介绍 L-798106 是强效且高度选择性的前列腺素类 EP3 受体拮抗剂 (Ki=0.3 nM),它在 EP4,EP1 和 EP2 受体上也具有微摩尔活性,Ki 值分别为 916 nM,>5000 nM 和 >5000 nM。
生物活性

L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has  micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively.

体外研究

L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses.
L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release.

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

Cell Viability Assay

Cell Line: Guinea-pig vas deferens
Concentration: 200 nM
Incubation Time:
Result: Showed an apparent pA2 of 7.48±0.25.

Cell Viability Assay

Cell Line: Guinea-pig tracheal smooth muscle
Concentration: 10 μM
Incubation Time:
Result: Attenuated significantly the inhibitory effect of all agents tested (in % inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 to 8.6; 8-iso-PGE2 from 51.6 to 9.2; PGE2 from 61.2 to 2.9; sulprostone from 55.9 to 18.8).
体内研究
(In Vivo)

L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice.

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

Animal Model: Male db/db mice
Dosage: 50 and 100 μg/kg
Administration: Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks
Result: Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice.
体内研究

L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice.

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

Animal Model: Male db/db mice
Dosage: 50 and 100 μg/kg
Administration: Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks
Result: Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice.
体内研究

L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice.

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

Animal Model: Male db/db mice
Dosage: 50 and 100 μg/kg
Administration: Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks
Result: Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice.
性状Solid
溶解性数据
In Vitro: 

DMSO : 10 mg/mL (18.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8641 mL 9.3207 mL 18.6414 mL
5 mM 0.3728 mL 1.8641 mL 3.7283 mL
10 mM 0.1864 mL 0.9321 mL 1.8641 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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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