2. GPCR/G Protein
  3. GPR84
  4. 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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PSB-16671

PSB-16671 Chemical Structure

CAS No. : 2094630-35-8

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PSB-16671 Related Antibodies

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Description

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[1][2][3].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.0415 μM
Compound: 9; PSB-16671
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
[PMID: 31721581]
In Vitro

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.

PSB-16671 Related Antibodies
Molecular Weight

318.27

Formula

C17H10F4N2
CAS No.
SMILES

FC1=CC2=C(NC=C2CC3=CNC4=C3C=C(F)C=C4F)C(F)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PSB-16671 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PSB-166712094630-35-8PSB16671PSB 16671GPR84G protein coupled receptor 84Flp-In T-REx 293 cellsCHO cellsβ-arrestin recruitmentmouse neutrophilsTHP-1 monocytesHEK293 cellsRAW264.7 macrophagesmacrophagesGi couplingInhibitorinhibitorinhibit

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