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LMPTP INHIBITOR 1 hydrochloride

产品编号 T4491 CAS 2310135-38-5

别名: LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base))

LMPTP INHIBITOR 1 hydrochloride 是一种高选择性的低分子量蛋白酪氨酸磷酸酶 (LMPTP) 抑制剂。LMPTP INHIBITOR 1 (hydrochloride) 能够抑制 LMPTP-A 的活性，IC50值为 0.8 μM。

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LMPTP INHIBITOR 1 hydrochloride Chemical Structure

LMPTP INHIBITOR 1 hydrochloride, CAS 2310135-38-5

规格	价格/CNY	货期
1 mg	￥ 1,780	现货
5 mg	￥ 4,480	现货
10 mg	￥ 6,380	现货
25 mg	￥ 9,620	现货
50 mg	￥ 12,900	6-8周
1 mL * 10 mM (in DMSO)	￥ 4,990	现货

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其他形式的 LMPTP INHIBITOR 1 hydrochloride:

LMPTP INHIBITOR 1 dihydrochloride
现货

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纯度: 99.63%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.
靶点活性	LMPTPA:0.8 μM
体外活性	LMPTP INHIBITOR 1 (hydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase, with an IC 50 of 0.8 μM for LMPTP-A. LMPTP INHIBITOR 1 shows more potent effect on LMPTP-A versus LMPTP-B. LMPTP inhibitor 1 (Compound 23; 10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes [1].
体内活性	LMPTP inhibitor 1 is orally bioavailable, and results in appr 680 nM mean serum concentration after treatment of 0.03% w/w, while treatment with 0.05% w/w results in >3 μM; which also reverses diabetes in obese mice. LMPTP inhibitor 1 (0.05% w/w) inhibits LMPTP activity, significantly improves glucose tolerance and reduces fasting insulin levels of diabetic DIO mice, without affecting body weight [1].
激酶实验	Phosphatase assays are performed in buffer containing 50 mM Bis-Tris, pH 6.0, 1 mM DTT and 0.01% Triton X-100 at 37°C. For assays conducted with 3-O-methylfluorescein phosphate (OMFP) as substrate, fluorescence is monitored continuously at λex = 485 and λem = 525 nm. For assays conducted with para-nitrophenyl phosphate (pNPP) as substrate, the reaction is stopped by addition of 2X reaction volume of 1 M NaOH, and absorbance is measured at 405 nm. IC50 values are determined from plots of LMPTP inhibitor 1 concentration versus percentage of enzyme activity. For inhibitor selectivity assays, each PTP is incubated with either 0.4 mM OMFP or 5 mM pNPP in the presence of 40 μM LMPTP inhibitor 1 or DMSO. Equal units of enzyme activity, comparable to the activity of 10 nM human LMPTP-A, are used. For the inhibitor reversibility assay, 50 nM human LMPTP-A is pre-incubated with 10 μM LMPTP inhibitor 1 or DMSO for 5 min. The enzyme is diluted 100X in phosphatase assay buffer containing 0.4 mM OMFP and fluorescence is measured at the indicated time points [1].
细胞实验	Human HepG2 cells are cultured in Eagle's Minimal Essential Medium (ATCC) containing 10% fetal bovine serum (FBS), 100 U/mL penicillin and 100 μg/mL streptomycin. The absence of Mycoplasma contamination in HepG2 cultures is confirmed using the Lonza MycoAlert Mycoplasma Detection Kit. Cells are treated with 10 μM LMPTP inhibitor 1 in serum-starvation media (0.1% FBS) overnight, following which cells are stimulated with 10 nM bovine insulin for 5 min at 37°C. For detection of IR tyrosine phosphorylation by immunoprecipitation/Western blotting, cells are lysed in radioimmunoprecipitation assay buffer containing 1 mM phenylmethylsulfonyl fluoride, 10 μg/mL aprotinin/leupeptin, 10 mM sodium orthovanadate, 5 mM sodium fluoride, and 2 mM sodium pyrophosphate, and the IR is immunoprecipitated using the anti-IRβ Ab. IR tyrosine phosphorylation of immunoprecipitates is determined by Western blotting with the anti-pIR/pIGFR-Y1162/Y1163 Ab [1].
动物实验	LMPTP inhibitor 1 is administered to male B6 or Acp1fl/fl albumin-Cre+ DIO mice at 0.05% w/w in high-fat diet (HFD) rodent chow. Control groups consist of male B6 or Acp1fl/fl albumin-Cre+ littermate mice administered HFD rodent chow alone. Mice are allowed food and water ad libitum and weighed daily. Randomization is not used in these experiments; rather littermate mice are assigned to treatment or control groups in a manner to maintain similar mean body weights between the 2 groups at the start of the study. Insulin-induced liver IR phosphorylation, IPGTT, and fasting insulin levels are assessed after treatment. Diabetic (displaying overnight [13 hr] fasting blood glucose levels ≥140 mg/dL) B6 DIO mice are used in experiments to assess IPGTT and fasting insulin levels [1].

别名	LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base))
分子量	481.07
分子式	C28H37ClN4O
CAS No.	2310135-38-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 9 mg/mL (18.71 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0787 mL	10.3935 mL	20.787 mL	51.9675 mL
	5 mM	0.4157 mL	2.0787 mL	4.1574 mL	10.3935 mL
	10 mM	0.2079 mL	1.0393 mL	2.0787 mL	5.1967 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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容积

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浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Stanford SM1, et al. Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase. Nat Chem Biol. 2017 Jun;13(6):624-632.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LMPTP INHIBITOR 1 hydrochloride 2310135-38-5 Metabolism Phosphatase LMPTP INHIBITOR 1 Hydrochloride LMPTP INHIBITOR 1 hydrochloride (1908414-82-3(free base)) Inhibitor inhibitor inhibit

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LMPTP INHIBITOR 1 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords