| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Danegaptide hydrochloride (GAP-134 and ZP-1609) is a novel, potent, selective and orally bioavailable small molecule gap-junction modifier with a potential for the treatment of atrial fibrillation.
| ln Vitro |
Danegaptide (GAP-134, Compound 9f; 0.01 nM-100 μM) is designed to decrease dye food in C6 neuroastroma cells that have been cultivated [1].
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| ln Vivo |
The effectiveness of diengaptide (GAP-134, compound 9f) was assessed in vivo using a CaCl2 mouse model. Danegaptide (GAP-134) is bioactive and decreases atrial fibrillation in a dog model. Danegaptide (GAP-134) in rats at a mean heart rate concentration of 250 nM considerably prolongs the ischemia state following infusion of CaCl2[1]. Heart rate, arterial blood pressure, and other electrocardiogram (ECG) parameters are unaffected by danegaptide. Danegaptide is a strong antiarrhythmic drug that causes arrhythmias brought on by reperfusion or cardiovascular disease in beagle dogs who have been given a barbiturate and made unconscious [2].
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| 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):908-11.
[2]. Elke De Vuyst, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83. |
| Molecular Formula |
C14H18CLN3O4
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| Molecular Weight |
327.7634
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| CAS # |
943133-81-1
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| Related CAS # |
Danegaptide;943134-39-2
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| SMILES |
O=C(O)[C@H]1N(C(CN)=O)C[C@H](NC(C2=CC=CC=C2)=O)C1.[H]Cl
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| Chemical Name |
(4R)-Glycyl-4-(benzoylamino)-L-proline hydrochloride
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| Synonyms |
Danegaptide GAP-134 HCl GAP-134-HCl GAP134HCl GAP 134 HCl GAP134 hydrochloride
GAP-134 hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 55 mg/mL (~167.81 mM)
H2O : ≥ 50 mg/mL (~152.55 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (305.10 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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