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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。
Bemesetron图片
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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.1826 mL15.9129 mL31.8258 mL
5 mM0.6365 mL3.1826 mL6.3652 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。