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Cat. No.: HY-189071

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AZD1386

AZD1386 is an orally active TRPV1 antagonist. AZD1386 blocks L-type calcium channels. AZD1386 can be used in pain research.

For research use only. We do not sell to patients.

CAS No.: 946080-23-5
Formula: C₁₉H₁₃ClF₃N₃O₃
Molecular Weight:423.78

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AZD1386 Chemical Structure

CAS No.: 946080-23-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

AZD1386 is an orally active TRPV1 antagonist. AZD1386 blocks L-type calcium channels. AZD1386 can be used in pain research^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

^[1]^[2]^[3]^[4]^[5]

TRPV1

L-type calcium channel

All TRP Channel Isoforms :

All Calcium Channel Isoforms :

In Vitro

AZD1386 is 0.5% free in dog plasma and 0.97% free in human plasma in the in vitro plasma protein binding assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cardiovascular Regulation

AZD1386 (100 mg/kg; oral; at least 3 days apart between doses) shortens the QTc interval in conscious Beagle dogs, with a maximum decrease of 25.8 ms from baseline at 100 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Beagle (N=6; weight 11-12.3 kg)^[1]
Dosage:

100 mg/kg
Administration:

oral; each dose at least 3 days apart
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

CAS No. 946080-23-5
Molecular Weight 423.78
Formula C₁₉H₁₃ClF₃N₃O₃
SMILES

O=C1NC(=O)C2(N1)C(=O)N(C=3C(=CC(Cl)=CC32)C)CC4=CC=CC(=C4)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

[2]. Trevisani M, et al. TRPV1 antagonists as analgesic agents.

[3]. Horoszok L, et al. Use of spiro[imidazolidine-4,3'-indole]-2,2',5'(1H)-triones for treatment of conditions associated with vanilloid receptor 1. WO 2007/091946 A1. 2007 Aug 16.

[4]. Möller KÄ, et al. TRPV1 antagonist for OA pain: preclinical in vivo results predict clinical outcome. Osteoarthritis and Cartilage. 2016 Apr 1;24:S456.

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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AZD1386

All TRP Channel Isoforms

All Calcium Channel Isoforms