[CAS NO. 943133-81-1] Danegaptide Hydrochloride
PRODUCTS SPECIFICATIONS [943133-81-1]
DESCRIPTION [943133-81-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 327.76 |
| Molecular Formula | C14H18ClN3O4 |
| SMILES | O=C(N[C@H]1CN(C(CN)=O)[C@H](C(O)=O)C1)C2=CC=CC=C2.[H]Cl |
1 Publications Citing Use of MCE
Summary
IC50 & Target
Gap junction.
In Vitro
Danegaptide (GAP-134, compound 9f; 0.01 nM-100 μM) dose dependently reduces dye uptake in cultured C6 glioma cells in a manner [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Danegaptide (GAP-134, compound 9f) is evaluated for in vivo efficacy in the mouse CaCl
2
model after oral administration. For doses of 5-20 mg/kg po, Danegaptide significantly prolongs the time to conduction block in mice after the infusion of CaCl
2
[1]
.
Danegaptide (GAP-134) is biologically active upon oral administration at an average plasma concentration of 250 nM, and reduces atrial fibrillation in a dog model. Danegaptide has no effect on heart rate, arterial blood pressure or other electrocardiogram (ECG) parameters. Danegaptide is an effective antiarrhythmic compound in the setting of ischaemia/reperfusion-induced arrhythmogenesis in barbiturate-anesthetized, open-chest beagles
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00543946 | Wyeth is now a wholly owned subsidiary of Pfizer |
Arrhythmia
|
October 2007 | Phase 1 |
| NCT00783341 | Wyeth is now a wholly owned subsidiary of Pfizer |
Healthy Subjects
|
November 2008 | Phase 1 |
| NCT01977755 | Zealand Pharma |
Focus of Study is STEMI
|
November 2013 | Phase 2 |
| NCT00510029 | Wyeth is now a wholly owned subsidiary of Pfizer |
Arrhythmia
|
September 2007 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 55 mg/mL ( 167.81 mM )
H 2 O : ≥ 50 mg/mL ( 152.55 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0510 mL | 15.2551 mL | 30.5101 mL |
| 5 mM | 0.6102 mL | 3.0510 mL | 6.1020 mL |
| 10 mM | 0.3051 mL | 1.5255 mL | 3.0510 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (305.10 mM); Clear solution; Need ultrasonic
References
- [1] John A Butera, et al. Discovery of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride (GAP-134)13, an orally active small molecule gap-junction modifier for the treatment of atrial fibrillation. J Med Chem. 2009 Feb 26;52(4):
- [2] Elke De Vuyst, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83.
Synonyms