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Cat. No.: HY-156953

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GPR183 antagonist-4

GPR183 antagonist-4 is a potent and selective GPR183 antagonist with an IC₅₀ of 8.31 nM. GPR183 antagonist-4 inhibits receptor activation-mediated calcium signaling by antagonizing GPR183, and exhibits efficacy in ameliorating neuropathic pain-related allodynia. GPR183 antagonist-4 is useful for research on GPR183 signaling and neuropathic pain.

For research use only. We do not sell to patients.

CAS No.: 1210803-60-3
Formula: C₁₉H₂₅N₃O₅
Molecular Weight:375.43

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

GPR183 antagonist-4 Chemical Structure

CAS No.: 1210803-60-3

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[1]

GPR183

In Vitro

GPR183 antagonist-4 (SAE-1) (preincubation for 15 min; 7α,25-OHC 200 nM) inhibits 7α,25-OHC-induced calcium mobilization in GPR183-expressing HL-60 cells with an IC₅₀ of 8.31 nM^[1].
GPR183 antagonist-4 alone does not induce calcium mobilization in HL-60 cells, whereas it exhibits antagonistic activity against 7α,25-OHC-induced GPR183-dependent calcium signaling^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SAE-1 (SAE-1) (800 nM; i.t.; acute) reverses mechanical allodynia in a time-dependent manner in the CCI model of male and female ICR mice, with no significant effect on contralateral mechanical sensitivity^[1].
GPR183 antagonist-4 (0.15-1.5 ng; i.th.; 5 μL; single administration on day 7 after CCI) reverses mechanical allodynia on the ipsilateral side in a time- and dose-dependent manner in a CCI-induced neuropathic pain rodent model, with no significant effect on contralateral paw withdrawal thresholds^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1210803-60-3
Molecular Weight 375.43
Formula C₁₉H₂₅N₃O₅
SMILES

O=C1N=C(NC(=C1CC(=O)NC(C2=CC(OC)=C(OC)C(OC)=C2)C)C)C
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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

Handling Instructions (2659 KB)

References

[1]. Salvemini D, et al. GPR183 Antagonists for the Treatment of Pain. US Patent Application Publication US20210122750A1. Published April 29, 2021. Applicant: Saint Louis University.

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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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