TRPV1 antagonist 11
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice.
For research use only. We do not sell to patients.
- CAS No.: 3084843-71-7
- Formula: C31H37N7O2
- Molecular Weight:539.67
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Opioid Receptor Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
TRPV1 29.3 nM (IC50) |
μ Opioid Receptor/MOR 60.3 nM (Ki) |
Chemical Information
-
CAS No. 3084843-71-7
-
Molecular Weight 539.67
-
Formula C31H37N7O2
-
SMILES
COC1=CC2=C(C(CCNC(N3CCN(CC3)C4=NC=CC(N5CCC(CC5)C6=CC=CC=C6)=N4)=O)=CN2)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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.
-
Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)