PSB-16671
PSB-16671 is an allosteric agonist of GPR84. PSB-16671 recruits β-arrestins and couples to Gi, enhances the Gi activation potency of orthosteric agonists, and exerts a synergistic effect with orthosteric agonists. PSB-16671 promotes G protein activation and partial chemotaxis independent of GPR84 in mouse neutrophils, maintains the phagocytic function of macrophages against cancer cells without inducing receptor desensitization. PSB-16671 can be used in cancer-related research.
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- CAS. Nr.: 2094630-35-8
- Formel: C17H10F4N2
- Molecular Weight:318.27
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.0415 μM
Compound: 9; PSB-16671
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Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method
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[PMID: 31721581] |
PSB-16671 is a target-specific allosteric agonist of human GPR84 expressed in Flp-In T-REx 293 cells, with a pEC50 of 6.28[1].
PSB-16671 is a target-specific allosteric agonist of mouse GPR84 expressed in Flp-In T-REx 293 cells, with a pEC50 of 6.53[1].
PSB-16671 is a target-specific agonist of endogenous human GPR84 in THP-1 monocytes, with similar potency in vehicle-treated (pEC50 = 6.82) and LPS (HY-D1056)-treated (pEC50 = 6.94) cells[1].
PSB-16671 is a target-specific agonist of endogenous murine GPR84 in RAW264.7 macrophages, with a pEC50 of 6.75[1].
PSB-16671 acts as a potent GPR84 agonist in CHO cells expressing GPR84, with an EC50 of 41.3 nM[2].
PSB-16671 induces β-arrestin recruitment in CHO cells expressing GPR84, with an EC50 of 5.47 μM[2].
PSB-16671 is a Gi-biased agonist-positive allosteric modulator (ago-PAM) of the human GPR84-Gi2α fusion protein expressed in Flp-In T-REx 293 cells, which directly activates the Gi signaling pathway with a pEC50 of -6.17 M[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2094630-35-8
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Molecular Weight 318.27
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Formel C17H10F4N2
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SMILES
FC1=CC2=C(NC=C2CC3=CNC4=C3C=C(F)C=C4F)C(F)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Mancini SJ, et al. On-target and off-target effects of novel orthosteric and allosteric activators of GPR84. Sci Rep. 2019;9(1):1861. Published 2019 Feb 12. [Content Brief]
[2]. Pillaiyar T, et al. Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84. J Med Chem. 2017;60(9):3636-3655. [Content Brief]
[3]. Zhang X, et al. Mechanism of GPR84 allosteric modulation at a helix 8-proximate site. bioRxiv [Preprint]. 2026 Apr 12:2026.04.10.715585. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PSB-16671 Related Classifications
HY-182723 Related Classifications
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