PF-04991532

Cat. No.: HY-100181 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

PF-04991532 Chemical Structure

CAS No. : 1215197-37-7

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 920	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Other Forms of PF-04991532:

(R)-PF-04991532 In-stock

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Description

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]

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].

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

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].

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

Clinical Trial

Molecular Weight

396.36

Formula

C₁₈H₁₉F₃N₄O₃

CAS No.

1215197-37-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(NC([C@@H](N2C=C(C(F)(F)F)N=C2)CC3CCCC3)=O)N=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (315.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2523 mL	1.2615 mL	2.5230 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (251 KB) Elemental Analysis Report (109 KB)

Handling Instructions (2659 KB)

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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 04991532Inhibitorinhibitorinhibit

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