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Otaplimastat
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。
Otaplimastat图片
CAS NO:1176758-04-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
SP-8203
产品介绍
Otaplimastat (SP-8203) 是一种基质金属蛋白酶 (MMP) 抑制剂,以竞争方式阻断NMDA受体介导的兴奋性毒性。Otaplimastat 还具有抗氧化活性。Otaplimastat 可用于脑缺血损伤的研究。
生物活性

Otaplimastat (SP-8203), amatrix metalloproteinase (MMP)inhibitor, blocksN-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury[1][2][3].

IC50& Target[1]

MMP

 

NMDA

 

体外研究
(In Vitro)

Otaplimastat (87.5-350 μM; 20 min) protects neuronal cells against NMDA-induced cell death in a competitive manner[1].
Otaplimastat (350 μM) inhibits Ca2+influx following activation of NMDA receptors in primary cultured neuron[1].
Otaplimastat (2-200 μM; pretreated for 4 h) significantly suppresses H2O2-induced cell death and reactive oxygen species production[2].

体内研究
(In Vivo)

Otaplimastat (10-20 mg/kg; i.p. 30 min before occlusion and 1 h after reperfusion) prevents ischemic neuronal death in the occlusion model of MCA[1].
Otaplimastat (5-10 mg/kg; i.p. daily for 10 days) attenuates impairment of stroke-induced motor function[2].

Animal Model:Male Wistar rats (280-310 g, 9 weeks) were induced transient middle cerebral artery (MCA) occlusion[1]
Dosage:10, 20 mg/kg
Administration:I.p. before 30 min and after an hour of the MCA-occlusion operation
Result:Significantly reduced infarct volume.
Improved spatial learning and memory impairments.
Clinical Trial
分子量

534.61

性状

Solid

Formula

C28H34N6O5

CAS 号

1176758-04-5

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 : 100 mg/mL(187.05 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8705 mL9.3526 mL18.7052 mL
5 mM0.3741 mL1.8705 mL3.7410 mL
10 mM0.1871 mL0.9353 mL1.8705 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。