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L-690,330

现货
Catalog No.
B5011
肌醇单磷酸酶(IMPase)的竞争性抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 3,696.00
Ship with 10-15 days

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Background

L-690,330 is a competitive inhibitor of inositol monophosphatase (IMPase) with a Ki value of between 0.2 and 2 μM depending on the source of IMPase [1].

In the phosphatidylinositol (PI) cycle cell signalling pathway, IMPase is involved as a key enzyme. Inositol monophosphates, inositol(1)phosphate [Ins(l)P], inositol(3)phosphate [Ins(3)P], and inositol(4)phosphate [Ins(4)P] are hydrolyzed by IMPase and produce free inositol. Free inositol can then be used to synthesize PI [1].

In carbachol-stimulated m1 CHO cells, the treatment with L-690,330 alone did not increase the amount of [3H]InsP1. In the absence of L-690,330, the treatment with carbachol alone increased levels of [3H]InsP1, resulted in levels ranging from 20 to 100% above basal [3H]InsP1 levels. In the presence of carbachol, lithium at 10 mM increased the amount of [3H]InsP1 by approximate five folds (relative to [3H]InsP1 levels in carbachol-stimulated cells) and the EC50 value of this effect was about 1 mM. In carbachol-stimulated cells, L-690,330 at 10 mM resulted in only ~40% of the maximum response seen in the case with lithium treatment [1].

In mouse brains, in the absence of L-690,330, pilocarpine produced approximately doubled levels of Ins(1)P. In the absence of pilocarpine, L-690,330 did not affect Ins(1)P levels. Under pilocarpine-stimulated conditions, treatment with L-690,330 resulted in a pronounced accumulation of Ins(1)P, with the maximum level observed 1 h after injection. The maximum was of an approximate four-fold elevation [1].

Reference:
[1].  Atack JR, Cook SM, Watt AP, et al. In Vitro and In Vivo Inhibition of Inositol Monophosphatase by the Bisphosphonate L-690,330. Journal of neurochemistry, 1993, 60(2): 652-658.

Chemical Properties

Physical AppearanceOff-white solid
StorageStore at RT
M.Wt298.13
Cas No.142523-38-4
FormulaC8H12O8P2
Solubility<29.81mg/ml in H2O
Chemical Name(1-(4-hydroxyphenoxy)ethane-1,1-diyl)diphosphonic acid
SDFDownload SDF
Canonical SMILESOP(O)(C(OC(C=C1)=CC=C1O)(C)P(O)(O)=O)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

M1 CHO细胞

制备方法

在无菌水中的溶解度为100 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.1 ~ 10 mM

实验结果

在Carbachol刺激的m1 CHO细胞中,单独使用L-690,330不增加[3H]InsP1水平;单独使用锂轻微增加[3H]InsP1水平;单独使用Carbachol使[3H]InsP1的量增加20 ~ 100%。

动物实验 [1]:

动物模型

Pilocarpine刺激的小鼠

给药剂量

0 ~ 1 mmol/kg;皮下注射

实验结果

在Pilocarpine刺激的小鼠中,L-690,330呈剂量依赖性地提升脑Ins(1)P水平,其ED50值为0.3 mmol/kg。注射L-690,330,于1小时后,L-690,330最大程度地提升Ins(1)P水平(约4倍)。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Atack JR, Cook SM, Watt AP, et al. In Vitro and In Vivo Inhibition of Inositol Monophosphatase by the Bisphosphonate L-690,330. Journal of neurochemistry, 1993, 60(2): 652-658.

质量控制

质量控制和MSDS

批次:

化学结构

L-690,330