2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. PF-04991532

PF-04991532 是一种有效的肝选择性葡萄糖激酶激活剂，在人类和大鼠中的 EC50 值分别为 80 和 100 nM。

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PF-04991532 Chemical Structure

PF-04991532 Chemical Structure

CAS No. : 1215197-37-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1188
In-stock
5 mg ￥1080
In-stock
10 mg ￥1890
In-stock
25 mg ￥3780
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of PF-04991532:

PF-04991532 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.

IC50 & Target

EC50: 80 nM (glucokinase in human), 100 nM (glucokinase in rat)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Hepatocyte EC50
0.19 μM
Compound: 19
Induction of glucokinase translocation from nucleus to cytoplasm in cryopreserved rat hepatocytes after 1 hr by Hoechst staining-based fluorescence microscopic analysis
Induction of glucokinase translocation from nucleus to cytoplasm in cryopreserved rat hepatocytes after 1 hr by Hoechst staining-based fluorescence microscopic analysis
[PMID: 22196621]
体外研究
(In Vitro)

PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 nM in human and 100 nM in rat and also a Phase 2 clinical candidate. Mechanistic experiments conducted in freshly isolated primary rat hepatocytes treated for 1 hour with PF-04991532 show increased 2-[14C]-deoxyglucose uptake (EC50 =1.261 µM) and increased glucose oxidation (EC50=5.769 µM). Additionally, PF-04991532 decreases the production of glucose from 1-[14C]-lactate in a dose dependent manner (EC50 =0.626 µM). In isolated rat hepatocytes, PF-04991532 increases the expression of G6Pase compare to cells treated only with 100 nM glucagon, and the greatest increase in G6Pase mRNA expression is in the presence of 25 mM glucose, 100 nM glucagon and PF-04991532[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PF-04991532 相关抗体:
体内研究
(In Vivo)

A single dose of PF-04991532 increases the glucose infusion rate in order to maintain hyperglycemia. Despite the elevations in plasma triglycerides, surprisingly, hepatic triglycerides in rats dosed with 19 days of PF-04991532 are identical to vehicle treated GK rats. In an additional cohort treated for 28 days, identical hepatic lipid concentrations are observed between vehicle and rats dosed with PF-04991532 (Vehicle: 9.89±0.31; PF-04991532 100 mg/kg: 9.91±0.31). In rats treated with PF-04991532, there is increased expression of lipogenic gene expression such as acetyl-CoA carboxylase (ACC), ATP citrate lyase (ACLY), and fatty acid synthase (FAS)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

396.36

Formula

C18H19F3N4O3
CAS 号
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (315.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5230 mL 12.6148 mL 25.2296 mL
5 mM 0.5046 mL 2.5230 mL 5.0459 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

COA (288 KB) 元素分析报告 (212 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Primary rat hepatocytes are used to determine the expression of G6Pase. 50,000 freshly isolated rat hepatocytes are incubated in Williams E media overnight supplemented with 100 nM dexamethasone, 1×ITS, and 1×PenStrep. The following morning the media is aspirated, and changed to DMEM no glucose media supplemented with either 5 mM glucose, 25 mM glucose, 1 µM insulin, 100 nM glucagon, or 10 µM PF-04991532. Following 2 hours the media is aspirated, washed twice, and 100 µL of RLT is added to the cells. RNA is extracted with a RNeasy kit[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

13 week old male Goto Kakizaki rats with in-dwelling carotid artery and jugular vein catheters are used in this study. Surgeries are performed one day before shipping. Upon arrival, animals are individually housed, allowed ad libitum chow, and acclimated to their new environment for 6 to 7 days. Animals are randomly assigned either a 100 mg/kg PF-04991532 treatment or vehicle control treatment and orally gavaged at 5 mL/kg. On the day of the experiment, 0.5% Methyl cellulose vehicle is used in vehicle-treated rats. Studies are performed in unstressed, awake, chronically catheterized rats using the insulin clamp technique, in combination with [3-3H] glucose. At the end of the in vivo studies, rats are euthanized[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

PF-04991532 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5230 mL 12.6148 mL 25.2296 mL 63.0740 mL
5 mM 0.5046 mL 2.5230 mL 5.0459 mL 12.6148 mL
10 mM 0.2523 mL 1.2615 mL 2.5230 mL 6.3074 mL
15 mM 0.1682 mL 0.8410 mL 1.6820 mL 4.2049 mL
20 mM 0.1261 mL 0.6307 mL 1.2615 mL 3.1537 mL
25 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5230 mL
30 mM 0.0841 mL 0.4205 mL 0.8410 mL 2.1025 mL
40 mM 0.0631 mL 0.3154 mL 0.6307 mL 1.5768 mL
50 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2615 mL
60 mM 0.0420 mL 0.2102 mL 0.4205 mL 1.0512 mL
80 mM 0.0315 mL 0.1577 mL 0.3154 mL 0.7884 mL
100 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6307 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-049915321215197-37-7PF04991532PF 04991532GlucokinaseHexokinase IVHexokinase DInhibitorinhibitorinhibit

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Inquiry Information

产品名称：
PF-04991532
目录号：
HY-100181
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