1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. TRP Channel Opioid Receptor
  3. 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.

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TRPV1 antagonist 11 Chemical Structure

TRPV1 antagonist 11 Chemical Structure

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Description

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[1].

IC50 & Target[1]

TRPV1

29.3 nM (IC50)

μ Opioid Receptor/MOR

60.3 nM (Ki)

Molecular Weight

539.67

Formula

C31H37N7O2

SMILES

COC1=CC2=C(NC=C2CCNC(N3CCN(CC3)C4=NC(N5CCC(CC5)C6=CC=CC=C6)=CC=N4)=O)C=C1

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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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TRPV1 antagonist 11
Cat. No.:
HY-176063
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