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PF-3716556 Proton Pump inhibitor

Name: PF-3716556
Brand: Selleck Chemicals
SKU: S2222
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S2222

PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na⁺,K⁺-ATPase, used for the treatment of gastroesophageal reflux disease.

Chemical Structure

Molecular Weight: 394.47

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Quality Control

Batch: Purity: 99.44%

99.44

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Other Proton Pump Inhibitors	Bafilomycin A1 (Baf-A1) Ilaprazole Tenatoprazole Ilaprazole sodium Revaprazan Hydrochloride Ufiprazole

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (197.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	394.47	Formula	C₂₂H₂₆N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	928774-43-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C2C(CCOC2=CC=C1)NC3=CC(=CN4C3=NC(=C4)C)C(=O)N(C)CCO

Mechanism of Action

Targets/IC₅₀/Ki	H+/K+-ATPase ~6.5(pIC50)
In vitro	PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of about of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro, displays no activity at Na+, K+-ATPase. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 has a competitive and reversible mode of action.
In vivo	PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 offers long-lasting and maximal efficacy within 30 min of a single dosing with responses that are maintained for at least 5 days of repeated dosing with no signs of tolerance.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18981288/

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