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Cat. No.: HY-184442

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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.

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Formule: C₁₉H₁₆Cl₂N₄O₃
Masse moléculaire:419.26

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GPR132 antagonist-2 Chemical Structure

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Use of MCE Products

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

Activité biologique
- Description
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

Description

In Vitro

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.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC
Mice^[1]	3 mg/kg	i.p.	785 ng/mL	30 min	64.4 min	109000 min·ng/mL

Chemical Information

Masse moléculaire 419.26
Formule C₁₉H₁₆Cl₂N₄O₃
SMILES

ClC(C(Cl)=C1)=CC=C1NC(C2=CC=NC(NC(CC3=C(C)ON=C3C)=O)=C2)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Hernandez-Olmos V, et al. First Structure-Activity-Relationship Study of Potent G2A Antagonists. Journal of medicinal chemistry. 2026 Jun 25;69(12):14309-14332. [Content Brief]

Calculators

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Calculateur de dilution

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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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MOQ

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100 mg

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