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(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor(D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
MRS5663 (Compound 3a) is an A3AR agonist, with an EC50 of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model .
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) can activate Gαi1 (EC50=0.8 nM) and recruit β-arrestin2 (EC50=31 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) exhibits prolonged cardiac effects .
A3AR agonist 2 (Compound 19) a selective A3AR agonist (Ki: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC50 value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions . A3AR agonist 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Noncatechol agonist-1 (19) is a Noncatechol agonist with full efficacy at both D1R-G protein and D1R-β-arrestin2 pathways, with pEC50 values of 8.41 for D1R-mediated cAMP production and 7.7 for β-arrestin2 recruitment, respectively .
VUF11207 (Compound 29) TFA is a CXCR7 agonist (pKi of 8.1) that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca 2+ release [2].
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC50=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC50 values in the range of 10-22 nM .
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
A3AR agonist 1 (Compound 12) is an A3AR agonist (Ki: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC50 value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc .
Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide [2] .
KOR agonist 3 (Compound 5) is a κ opioid receptor (κOR) agonist with an EC50 of 0.88 nM. KOR agonist 3 also has a certain activation effect on μOR with an EC50 of 720 nM. KOR agonist 3 shows no agonist activity for δOR at concentrations less than 1 μM. KOR agonist 3 has a lower ability to induce the recruitment of β-Arrestin-2 than U50488 (HY-15997B) .
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis [2].
SLW131 (Compound 10) is the antagonist for CCR7 with a good affinity of Ki of 9.85 nM. SLW131 inhibits CCL19-induced Go protein activation with an IC50 of 29.4 μM, inhibits β-arrestin2 recruitment with an IC50 of 6.0 μM. SLW131 inhibits CCL19-induced cell morphological changes in primary BMDCs, and CCR7-mediated migration in mouse CD4+ T cell .
FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2(FFA2/GPR43) with an EC50 of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC50 of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating
peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research .
Indacaterol xinafoate is an orally active long-acting β2-adrenergic agonist (LABA) with bronchodilatory effect. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol xinafoate can be utilized in asthma research [2].
Indacaterol acetate is an orally active ultra-long-acting β2 adrenergic receptor(ADRB2) agonist. Indacaterol acetate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol acetate can also be used in cardiovascular disease research [2].
Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor(ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research [2].
Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor(ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research [2].
Indacaterol (Standard) is the analytical standard of Indacaterol. This product is intended for research and analytical applications. Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor(ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research [2].
Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor(ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research [2].
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity [2].
UNC9975 is a D2R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research .
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity [2].
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[ 35S]GTPγSbinding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors [2] .
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases .
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity [2].
Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity [2].
AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca 2+ release [2].
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity [2].
Arrestin-β-2 Antibody (YA5111) is a mouse-derived and non-conjugated monoclonal antibody, targeting to Arrestin-β-2. It can be applicated for WB, ICC/IF assays, in the background of human, mouse, rat, pig.
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