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Testing Data (PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 +/- 0.112, 6.038 +/- 0.039 and 6.009 +/- 0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. 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. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in na¯ve tissues, cell lines and transfectants. [1])

PF 3716556, inhibitor

PF 3716556

Purity
>99%
Synonyms
PF 3716556; inhibitor
Ordering
For Research Use Only!
Purity/Purification
>99%
Solubility
Unknown
Formula
C22H26N4O3
CAS Number
928774-43-0
Preparation and Storage
Store at -20 degree C for 2 years.

Testing Data

(PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 +/- 0.112, 6.038 +/- 0.039 and 6.009 +/- 0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. 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. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in na¯ve tissues, cell lines and transfectants. [1])

Testing Data (PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 +/- 0.112, 6.038 +/- 0.039 and 6.009 +/- 0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. 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. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in na¯ve tissues, cell lines and transfectants. [1])
Related Product Information for PF 3716556, inhibitor
PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 +/-0.112, 6.038 +/-0.039 and 6.009 +/-0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. 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. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in naïve tissues, cell lines and transfectants. [1]
References
[1] Mori H et al. J Pharmacol Exp Ther. 2009 Feb; 328(2):671-9. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.

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Product Notes

The PF 3716556 (Catalog #AAA8506512) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "PF 3716556, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

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