TRPV1 antagonist 9
TRPV1 antagonist 9 (compound 13c) is an orally active transient receptor potential vanilloid 1 (TRPV1) channel antagonist. TRPV1 antagonist 9 blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors with IC50 values are 0.6 and 0.8 nM for Capsaicin (HY-10448) and acid-induced Ca2+ uptake, respectively. TRPV1 antagonist 9 blocks Capsaicin (HY-10448)-induced flinch response and causes hyperthermia in rats.
For research use only. We do not sell to patients.
- CAS No.: 939040-79-6
- Formula: C22H19F3N6O3
- Molecular Weight:472.42
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.6 nM
Compound: 13c
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Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx
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[PMID: 18386885] |
| CHO | IC50 |
0.8 nM
Compound: 13c
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Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx
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[PMID: 18386885] |
Chemical Information
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CAS No. 939040-79-6
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Molecular Weight 472.42
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Formula C22H19F3N6O3
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SMILES
NC1=NC(C(NC1=O)=CC=C2)=C2OC3=NC(NCCOC)=NC(C4=CC=C(C(F)(F)F)C=C4)=C3
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRPV1 antagonist 9 Related Classifications
HY-110091 Related Classifications
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