Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H26N4O3 |
Molecular Weight | 394.4668 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(CCO)C(=O)C1=CN2C=C(C)N=C2C(N[C@@H]3CCOC4=CC=CC(C)=C34)=C1
InChI
InChIKey=YBHKBMJREUZHOV-QGZVFWFLSA-N
InChI=1S/C22H26N4O3/c1-14-5-4-6-19-20(14)17(7-10-29-19)24-18-11-16(22(28)25(3)8-9-27)13-26-12-15(2)23-21(18)26/h4-6,11-13,17,24,27H,7-10H2,1-3H3/t17-/m1/s1
Molecular Formula | C22H26N4O3 |
Molecular Weight | 394.4668 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18981288
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18981288
PF-03716556 is a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. PF-03716556 inhibits the porcine, canine, and human recombinant gastric H+,K+-ATPase in a competitive manner without any biologically relevant activity against other tested receptors, ion channels, and enzymes, including the Na+,K+-ATPase. PF-03716556 inhibits gastric acid secretion in a dose-dependent manner in Ghosh-Schild rats and Heidenhain pouch dogs, producing full efficacy on treatment day 1. PF-03716556 is used for the treatment of gastroesophageal reflux disease.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2095173 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18981288 |
6.0 null [pIC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18981288
Rats: Intraduodenal administration of PF-03716556 inhibited gastric acid secretion in a dose-dependent manner over concentrations ranging from 1 to 10 mg/kg. Complete inhibition was observed at 10 mg/kg PF-03716556.
Heidenhain Pouch Dogs:Dose-dependent inhibition of gastric acid secretion was observed following oral administration of PF-03716556 at doses ranging from 0.3 to 3 mg/kg; complete inhibition was observed at 3 mg/kg
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18981288
In porcine ion-tight membrane vesicles, PF-03716556 inhibited
H,K-ATPase activity in a concentration-dependent
manner, with a pIC50 value of 7.095 at pH 7.4
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:37:13 GMT 2023
by
admin
on
Sat Dec 16 09:37:13 GMT 2023
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Record UNII |
701L6668UD
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Record Status |
Validated (UNII)
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Record Version |
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