All AbMole products are for research use only, cannot be used for human consumption.
PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026, 6.038 and 6.009 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 naive tissues, cell lines and transfectants.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | rat |
| Formulation | 5% DMSO and 15% Cremophor EL |
| Dosages | 1–10 mg/kg; 1 ml/kg |
| Administration | i.v. |
| Molecular Weight | 394.47 |
| Formula | C22H26N4O3 |
| CAS Number | 928774-43-0 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Potassium Channel Products |
|---|
| VU0810464
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration. |
| QO 58
QO 58 is a potent modulator of K(v)7 channels. |
| NS3623
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. |
| ML67-33
ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. |
| A-935142
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
