AZD1386
AZD1386 is an orally active TRPV1 antagonist. AZD1386 blocks L-type calcium channels. AZD1386 can be used in pain research.
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- No. CAS: 946080-23-5
- Fòrmula: C19H13ClF3N3O3
- Peso molecular:423.78
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
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TRPV1 |
L-type calcium channel |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle (N=6; weight 11-12.3 kg)[1]
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Dosage:100 mg/kg
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Administration:oral; each dose at least 3 days apart
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Result:Shortened the QTc interval in dogs.
The maximum effect was a 25.8 ms decrease from baseline, observed 1 hour after dosing at 100 mg/kg.
The dog population PD linear slope was 0.6 ms/µM/L (SE 0.2), with between-subject variability of 77%.
Increases in blood pressure and heart rate were also reported.
Chemical Information
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No. CAS 946080-23-5
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Peso molecular 423.78
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Fòrmula C19H13ClF3N3O3
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SMILES
O=C1NC(=O)C2(N1)C(=O)N(C=3C(=CC(Cl)=CC32)C)CC4=CC=CC(=C4)C(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Parkinson J, et al. Translational pharmacokinetic-pharmacodynamic modeling of QTc effects in dog and human. Journal of pharmacological and toxicological methods. 2013;68(3):357-66. [Content Brief]
[2]. Trevisani M, et al. TRPV1 antagonists as analgesic agents. [Content Brief]
[5]. Möller KÄ, et al. Using gait analysis to assess weight bearing in rats with Freund׳ s complete adjuvant-induced monoarthritis to improve predictivity: interfering with the cyclooxygenase and nerve growth factor pathways. European journal of pharmacology. 2015 Jun 5;756:75-84. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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