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PF-06409577

产品编号 T4427 CAS 1467057-23-3

别名: PF 06409577

PF-06409577 是一种具有口服活性的特异性 AMPK 变构激活剂，对α1β1γ1的EC50值为7 nM。

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PF-06409577, CAS 1467057-23-3

规格	价格/CNY	货期
1 mg	￥ 242	现货
2 mg	￥ 338	现货
5 mg	￥ 578	现货
10 mg	￥ 980	现货
25 mg	￥ 1,980	现货
50 mg	￥ 2,970	现货
100 mg	￥ 4,480	现货
500 mg	￥ 9,360	现货
1 mL * 10 mM (in DMSO)	￥ 613	现货

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纯度: 98.16%

纯度: 95.17%

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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	PF-06409577 is an effective, orally active, and specific allosteric activator of AMPK (EC50: 7 nM, for α1β1γ1).
靶点活性	AMPK α1β1γ1:7 nM (EC50)
体外活性	In human and rat , PF-06409577 has similar effectiveness for α1β1γ1 isoforms. PF-06409577 exhibits minimal off-target effects on a panel of receptors, ion channels, PDEs, and kinases. PF-06409577 has no inhibition of hERG in a patch-clamp assay (100 μM) and is not an inhibitor (IC50>100 μM) of the microsomal activities of major human cytochrome P450 isoforms[1].
体内活性	In rats, monkeys, and dogs, PF-06409577 has moderate plasma clearance and is well distributed with steady-state distribution volume. Following oral administration of crystalline PF-06409577 in 0.5% methylcellulose suspension, PF-06409577 is rapidly absorbed in dogs, rats, and monkeys. The corresponding oral bioavailability values in rats, monkeys, and dogs are 15%, 59%, and 100%, respectively. Dose-dependent increases in pAMPK relative to total AMPK (tAMPK) in whole kidney tissue are observed with a maximal 3.8-fold response at 300 mg/kg PF-06409577 treatment[1]. Oral administration of PF-06409577 (10, 30, and 100 mg/kg every day) resulted in dose-dependent reductions in proteinuria in the obese ZSF1 animals, with greater than 2-fold reduction in 24-hour urinary albumin loss compared with vehicle control after 60 days of treatment [2].
激酶实验	PF-06409577 is prepared in DMSO. PF-06409577 is incubated with fully phosphorylated AMPK in assay buffer at room temperature for 15 min followed by addition of PP2a and another incubation for 60 min at room temperature. The phosphatase treatment is quenched and the kinase assay initiated with the addition of okadaic acid (50 nM final), 50 nM Cy-5 SAMS peptide and ATP equal to Km for each isoform. Reactions are incubated for an additional 60 min and the kinase reaction is quenched with the addition of 10 mM EDTA and 2 nM Eu-pACC antibody in detection Buffer. Kinase activity is monitored by excitation at 320 nM and measuring emission at 665 and 615 nM, respectively[2].
动物实验	PF-06409577 is prepared in 0.5% methylcellulose[2].Daily administration of 0.5% methylcellulose (p.o.), PF-06409577 at 10, 30, or 100 mg/kg (p.o.), PF- 249 at 3, 10, or 30 mg/kg (p.o.), or ramipril in drinking water (1 mg/kg/day) is initiated and continued for 68 days. Urine is collected for 24-hours and volume recorded from all lean and obese rats after 14, 28, 42, and 60 days of dosing. On Day 63 all rats are administered a final dose after 16-hour overnight fasting. One hour following the final dose, blood glucose is measured by glucometer and a 100 μL tail vein blood sample collected and processed for determination of insulin levels and total protein. Each rat is then anesthetized with isoflurane. The right kidney is collected and immediately freeze-clamped and transferred to liquid nitrogen storage; the left kidney is fixed in 10% formalin. Rats are then euthanized by exsanguination from the vena cava[2].

别名	PF 06409577
分子量	341.79
分子式	C19H16ClNO3
CAS No.	1467057-23-3

存储

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

溶解度

Ethanol: 6.8 mg/mL(20 mM)

DMSO: 34.2 mg/mL(100 mM)

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.9258 mL	14.6289 mL	29.2577 mL	73.1443 mL
	5 mM	0.5852 mL	2.9258 mL	5.8515 mL	14.6289 mL
	10 mM	0.2926 mL	1.4629 mL	2.9258 mL	7.3144 mL
	20 mM	0.1463 mL	0.7314 mL	1.4629 mL	3.6572 mL
DMSO	50 mM	0.0585 mL	0.2926 mL	0.5852 mL	1.4629 mL
DMSO	100 mM	0.0293 mL	0.1463 mL	0.2926 mL	0.7314 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Cameron K O, Kung D W, Kalgutkar A S, et al. Discovery and preClinicalal characterization of 6-chloro-5-[4-(1-hydroxycyclobutyl) phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577), a direct activator of adenosine monophosphate-activated protein kinase (AMPK), for the potential treatment of diabetic nephropathy[J]. Journal of medicinal chemistry, 2016, 59(17): 8068-8081. 2. Salatto C T, Miller R A, Cameron K O, et al. Selective activation of AMPK β1-containing isoforms improves kidney function in a rat model of diabetic nephropathy[J]. Journal of Pharmacology and Experimental Therapeutics, 2017, 361(2): 303-311.

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

PF-06409577 1467057-23-3 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK Inhibitor AMP-activated protein kinase inhibit PF 06409577 PF06409577 inhibitor

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PF-06409577

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