Danegaptide |
| Catalog No.GC35806 |
Le danegaptide (GAP-134) est un modificateur de jonction lacunaire puissant, sélectif et actif par voie orale avec un effet antiarythmique.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 943134-39-2
Sample solution is provided at 25 µL, 10mM.
Danegaptide (GAP-134), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. Gap junction.
Gap junction uncoupling can alter conduction pathways and promote cardiac re-entry mechanisms that potentiate many supraventricular arrhythmias, such as atrial fibrillation (AF) and atrial flutter (AFL). Gap junction modifier Danegaptide (GAP-134), showed consistent efficacy on measures of conduction and AF/AFL inducibility in the canine sterile pericarditis model. Danegaptide (GAP-134) is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy, as already confirmed in phase I clinical trials.
[1]. De Vuyst E, Boengler K, Antoons G, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83. [2]. Laurent G, Leong-Poi H, Mangat I, et al. Effects of chronic gap junction conduction-enhancing antiarrhythmic peptide GAP-134 administration on experimental atrial fibrillation in dogs. Circ Arrhythm Electrophysiol. 2009 Apr;2(2):171-8. [3]. Hennan JK, Swillo RE, Morgan GA, et al. GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14. [4]. Rossman EI, Liu K, Morgan GA, et al. The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33. [5]. Eugene L. Piatnitski Cheklera, John A. Buterab, Li Dib, Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters. 2009,19(16): 4551-4554
| Cas No. | 943134-39-2 | SDF | |
| Canonical SMILES | O=C(N[C@H]1CN(C(CN)=O)[C@H](C(O)=O)C1)C2=CC=CC=C2 | ||
| Formula | C14H17N3O4 | M.Wt | 291.3 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4329 mL | 17.1644 mL | 34.3289 mL |
| 5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL |
| 10 mM | 0.3433 mL | 1.7164 mL | 3.4329 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
ZP1609 promotes GJs-CX43 expression and reconstitutes GJ-mediated astrocyte network, and inhibits the infammatory response of primary astrocytes after receiving a long-term isofurane anesthesia. ZP1609 alleviated long-term isofurane exposure-induced increased levels of IL-1β (k) and IL-6 (l) in primary astrocytes.
Mice were treated with Danegaptide (ZP1609) (dosage: 300µg/kg every time, three times/day) (GLPBIO, USA) by intraperitoneal injection for 3 consecutive days after the mice model was established.
Journal of Neuroinflammation 19.1 (2022): 1-22. PMID: 35255943 IF: 8.3222 -
Related Biological Data
Enhanced gap junctions Connexin43 coupling can alleviate cognitive dysfunction induced by long-term isoflurane anesthesia. Cognitive functions are impaired in mice after long-term isoflurane anesthesia and treatment with Danegaptide significantly improved the contextual fear memory (A).
After 30min of treatment with Danegaptide (ZP1609) (1μg/ml, GLPBIO, USA), the total Cx43 notably decreased in isoflurane-treated primary astrocytes and was not reversed by Danegaptide.
CNS Neuroscience & Therapeutics (2022). PMID: 36153812 IF: 7.0348
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *