Azidothiorphan
Azidothiorphan is an irreversible photoaffinity ligand and Endopeptidase 24.11 inhibitor, with a Ki value of 0.75 nM against Endopeptidase 24.11. Upon UV irradiation, Azidothiorphan binds to the active site of enkephalinase, resulting in irreversible loss of enzyme activity. Azidothiorphan produces long-lasting analgesic effects in mice. Azidothiorphan can be used in pain-related research.
For research use only. We do not sell to patients.
- CAS No.: 83960-29-6
- Formula: C12H14N4O3S
- Molecular Weight:294.33
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Azidothiorphan (100 nM; 5 minutes) irreversibly inhibits enkephalinase from mouse striatal membranes (P2 fraction) with 98% activity loss at 100 nM after 5 minutes of 254 nm irradiation[1].
Azidothiorphan potently inhibits purified neutral endopeptidase 24.11 with a Ki of 0.75 nM and acts as an active-site-directed irreversible photoaffinity ligand for the enzyme[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 83960-29-6
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Molecular Weight 294.33
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Formula C12H14N4O3S
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SMILES
[N-]=[N+]=NC1=CC=C(C=C1)CC(C(=O)NCC(=O)O)CS
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Roques BP, et al. New enkephalinase inhibitors as probes to differentiate "enkephalinase" and angiotensin-converting-enzyme active sites. Life Sci. 1982 Oct 18-25;31(16-17):1749-52. [Content Brief]
[2]. Beaumont A, et al. Irreversible photolabeling of active site of neutral endopeptidase-24.11 "enkephalinase" by azidothiorphan and [14C]-azidothiorphan. Molecular pharmacology. 1987 Nov;32(5):594-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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