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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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화학식: C₁₉H₁₆Cl₂N₄O₃
분자량:419.26

보관:

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

Data Sheet (267 KB)

GPR132 antagonist-2 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

분자량 419.26
화학식 C₁₉H₁₆Cl₂N₄O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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