Danegaptide
Based on 2 publication(s) in Google Scholar
Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.
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- CAS No.: 943134-39-2
- 화학식: C14H17N3O4
- 분자량:291.30
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Danegaptide
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Biological Activity
Gap junction.
Danegaptide (GAP-134, compound 9f; 0.01 nM-100 μM) dose dependently reduces dye uptake in cultured C6 glioma cells in a manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 943134-39-2
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분자량 291.30
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화학식 C14H17N3O4
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SMILES
O=C(N[C@H]1CN(C(CN)=O)[C@H](C(O)=O)C1)C2=CC=CC=C2
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Synonyms
GAP-134; ZP 1609
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Exp Neurol
Roles of astrocytic Connexin 43 gap junctional deficit in alpha-synucleinopathy and inflammation relevant to Parkinson's. [Abstract]2026 Jun 26:115897. PMID: 42362037 -
Lab Invest
Bioglass promotes wound healing by inhibiting endothelial cell pyroptosis through regulation of the connexin 43/reactive oxygen species (ROS) signaling pathway. [Abstract]2022 Jan;102(1):90-101. PMID: 34521991
순도&문서
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): [Content Brief]
[2]. Elke De Vuyst, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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