GR 113808

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GR 113808

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

144625-51-4

GR 113808 是一种有效且高度选择性的5-HT₄receptor受体拮抗剂 (pK_b= 8.8)。GR 113808 的选择性是 5-HT_1A，5-HT_1B，5-HT_2A，5-HT_2C和 5-HT₃受体的 300 倍。

生物活性

GR 113808 is a potent and highly selective5-HT₄ receptorantagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2Cand 5-HT₃receptors^[1].

IC₅₀& Target^[1]

5-HT₄Receptor

5-HT_1AReceptor

5-HT₃Receptor

5-HT_2AReceptor

5-HT_2CReceptor

体内研究
(In Vivo)

GR113808 (intraperitoneal injection; 1 mg/kg; 5-7 days starting 24 h after induction of colitis) shows a significant increase in the disease activity index (DAI),which includes evaluation of weight loss, stool consistency, and presence of fecal blood^[2].

Animal Model:	Mice^[1]
Dosage:	1 mg/Kg
Administration:	Intraperitoneal injection; 1 mg/Kg; 5-7 days starting 24 h after induction of colitis
Result:	Blocked protective effects of tegaserod after induction of colitis.

分子量

393.50

性状

Solid

Formula

C₁₉H₂₇N₃O₄S

CAS 号

144625-51-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 39 mg/mL(99.11 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.5413 mL	12.7065 mL	25.4130 mL
5 mM	0.5083 mL	2.5413 mL	5.0826 mL
10 mM	0.2541 mL	1.2706 mL	2.5413 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。