Otaplimastat

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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。

CAS NO:

1176758-04-5

SP-8203

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

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.8705 mL	9.3526 mL	18.7052 mL
5 mM	0.3741 mL	1.8705 mL	3.7410 mL
10 mM	0.1871 mL	0.9353 mL	1.8705 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。