Bemesetron

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Bemesetron

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:

40796-97-2

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议
100mg	电议

产品名称

MDL 72222

产品介绍

Bemesetron (MDL 72222) 是一种选择性5-HT₃受体拮抗剂，IC₅₀为 0.33 nM 。具有神经保护作用。

生物活性

Bemesetron (MDL 72222) is a selective5-HT₃receptorantagonist with anIC₅₀of 0.33 nM^[1]. Neuroprotective effect^[2].

IC₅₀& Target^[1]

5-HT₃Receptor

0.33 nM (IC₅₀)

体外研究
(In Vitro)

Blockade of 5-HT₃receptor with Bemesetron (MDL7222) reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Bemesetron (0.01, 0.1 and 1 μM, 15 hours) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H₂O₂-induced decrease of MTT reduction showing 74.9±2.4 and 79.0 ±2.5% with 1 μM and 5 μM, respectively, which are maximal effects^[2].
Pretreatment (20 minutes) with Bemesetron (1 μM), Y25130 (5 μM) or MK-801 (10 μM) significantly, but not completely, inhibits the H₂O₂-induced elevation of [Ca²⁺]_c^[2].
Bemesetron (1 μM, 15 hours) significantly blocks the H₂O₂-induced increase of caspase-3 immunoreactivity^[2].

Cell Viability Assay^[2]

Cell Line:	Primary cortical neuronal cells
Concentration:	0.01-1 μM
Incubation Time:	20 minutes (pretreatment); 15 hours (post-incubation)
Result:	Concentration-dependently reduced the H₂O₂-induced decrease of MTT reduction showing 74.9±2.4% with 1 μM, which was maximal effect.

Western Blot Analysis^[2]

Cell Line:	Primary cortical neuronal cells
Concentration:	1 μM
Incubation Time:	15 hours
Result:	Blocked significantly the H₂O₂-induced increase of caspase-3 immunoreactivity.

体内研究
(In Vivo)

Bemesetron (0.1, 1 and 10 mg/kg; i.p.) is used in male adult albino mice. The lowest dose do not cause any significant change in catalepsy. However, Bemesetron (1 mg/kg) causes a significant reduction of catalepsy (from 90 min after Haloperidol), while 10 mg/kg significantly potentiates the phenomenon (from 60 min after Haloperidol). The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximum potentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol^[3].

Animal Model:	Male adult albino mice, weighing 26-36 g^[3]
Dosage:	0.1-10 mg/kg
Administration:	Intraperitoneally injected, 20 min (pretreatment) +180 min (treatment)
Result:	Reduced catalepsy significantly at a dose of 1 mg/kg, whilst 10 mg/kg potentiated the phenomenon and 0.1 mg/kg was found to be without effect.

分子量

314.21

性状

Solid

Formula

C₁₅H₁₇Cl₂NO₂

CAS 号

40796-97-2

中文名称

贝美司琼

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 : 2 mg/mL(6.37 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.1826 mL	15.9129 mL	31.8258 mL
5 mM	0.6365 mL	3.1826 mL	6.3652 mL
10 mM	---	---	---

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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。