GPR132 antagonist-2
GPR132 antagonist-2 is a G2A (GPR132) antagonist with an IC50 of 0.69 μM. GPR132 antagonist-2 exerts weak stabilizing effects on the bromodomain of BRD2 and exhibits selectivity for non-olfactory GPCRs. GPR132 antagonist-2 inhibits G2A activation, blocks downstream inositol monophosphate accumulation, reverses G2A-mediated TRPV1 sensitization, suppresses 9-HODE-mediated capsaicin-induced TRPV1 responses, and activates FPR3. GPR132 antagonist-2 can be used in studies related to neuropathic pain.
For research use only. We do not sell to patients.
- Formula: C19H16Cl2N4O3
- Molecular Weight:419.26
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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
GPR132 antagonist-2 (Compound 65) at 20 μM exhibits weak binding to BET bromodomains, and shows low thermostabilizing effects on BRDT, BRD2, BRD3 and BRD4 proteins at the concentration of 20 μM[1].
GPR132 antagonist-2 does not activate G2A, and exhibits weak off-target activation against several GPCRs including FPR3 at a concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC |
|---|---|---|---|---|---|---|
| Mice[1] | 3 mg/kg | i.p. | 785 ng/mL | 30 min | 64.4 min | 109000 min·ng/mL |
Chemical Information
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Molecular Weight 419.26
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Formula C19H16Cl2N4O3
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SMILES
ClC(C(Cl)=C1)=CC=C1NC(C2=CC=NC(NC(CC3=C(C)ON=C3C)=O)=C2)=O
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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