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Cat. No.: HY-165466

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Azidothiorphan

Azidothiorphan is an irreversible photoaffinity ligand and Endopeptidase 24.11 inhibitor, with a K_i 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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Please store the product under the recommended conditions in the Certificate of Analysis.

Azidothiorphan Chemical Structure

CAS No.: 83960-29-6

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

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 K_i 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. .

In Vivo

Azidothiorphan (50 μg/mouse; intracerebroventricular injection) produces a long-lasting analgesic effect in mice, which does not disappear until 6 h later^[1].

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

Chemical Information

CAS No. 83960-29-6
Molecular Weight 294.33
Formula C₁₂H₁₄N₄O₃S
SMILES

[N-]=[N+]=NC1=CC=C(C=C1)CC(C(=O)NCC(=O)O)CS
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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]. 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]

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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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