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MDL-29951

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Chemical Structure| 130798-51-5 同义名 : -
CAS号 : 130798-51-5
货号 : A545278
分子式 : C12H9Cl2NO4
纯度 : 98%
分子量 : 302.11
MDL号 : MFCD00897722
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(165.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The N-methyl-D-aspartate receptor (NMDAR) is involved in normal physiological and pathological states in the brain[3]. The NMDA-preferring glutamate receptor subtype possesses, in addition to the recognition site for glutamate, a binding site for glycine. MDL-29951 is a novel glycine antagonist of NMDA receptor activation with a Ki value of 0.14 μM. It is approximately 2000-fold selective for the glycine binding site over the glutamate recognition sites. MDL-29951 completely inhibited the use-dependent binding of [3H]N-[1-(2-thienyl) cyclohexyl]-piperidine and was noncompetitive, glycine-reversible inhibitor of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations[4]. In addition, MDL-29951 was found to inhibit the human F16Bpase (Fructose-1,6-bisphosphatase; one of the rate limiting enzymes of hepatic gluconeogenesis) with an IC50 of 2.5 μM[5]. Moreover, MDL-29951 diminished myelination in primary oligodendrocytes isolated from heterozygous mice[6]. MDL-29951 was potent anticonvulsants after their i.c.v. administration to audiogenic seizure-susceptible DBA/2J mice[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.55mL

3.31mL

1.66mL

33.10mL

6.62mL

3.31mL
参考文献

[1]Wright SW, Carlo AA, et al. 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. Bioorg Med Chem Lett. 2003 Jun 16;13(12):2055-8.

[2]Baron BM, Harrison BL, et al. Potent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. J Pharmacol Exp Ther. 1992 Sep;262(3):947-56.

[3]Anti-NMDAR Autoimmune Encephalitis

[4]Potent Indole- And Quinoline-Containing N-methyl-D-aspartate Antagonists Acting at the Strychnine-Insensitive Glycine Binding Site

[5]3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic Acid: An Allosteric Inhibitor of fructose-1,6-bisphosphatase at the AMP Site

[6]Enigmatic GPCR Finds a Stimulating Drug