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β-arrestin assay

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標的別:	Adenosine Receptor (1) Apelin Receptor (APJ) (2) Arrestin (4) CXCR (1) Dopamine Receptor (4) Free Fatty Acid Receptor (1) GLP Receptor (1) GPR35 (1) GPR84 (1) Mas-related G-protein-coupled Receptor (MRGPR) (2) Opioid Receptor (1) PERK (1) Reference Standards (1)
研究分野別:	Cardiovascular Disease (1) Inflammation/Immunology (5) Metabolic Disease (3) Neurological Disease (7)
クリックケミストリー:	Alkynes (1)

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Targets Recommended: Biochemical Assay Reagents

製品番号	製品名	Target	研究分野	構造式

HY-160734

Aleniglipron GSBR-1290	GLP Receptor	Metabolic Disease
Aleniglipron (GSBR-1290) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist, with an EC₅₀ value of less than 0.1 nM in HDB cell lines in cAMP stimulation assays. Aleniglipron selectively activates the Gαs-cAMP signaling pathway of GLP-1R without β-arrestin recruitment. Aleniglipron induces insulin release, promotes glucose clearance, reduces food intake and decreases body weight. Aleniglipron is applicable to research related to type 2 diabetes and obesity .

HY-103254

ML221 5+ Cited Publications	Arrestin Apelin Receptor (APJ)	Neurological Disease
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the *β-arrestin* assay, and EC₈₀ of 10 nM in both assays.

HY-120878

CXCR2-IN-2 1 Publications Verification	CXCR	Inflammation/Immunology
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC₅₀=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC₅₀ of 0.04 μM .

HY-128121

MLS1547	Dopamine Receptor	Neurological Disease
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (K_i=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC₅₀=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC₅₀=9.9 μM) .

HY-119486A

(Rac)-Tavapadon (Rac)-PF-06649751; (Rac)-CVL-751	Dopamine Receptor Arrestin	Neurological Disease
(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 .

HY-178793

MrgprX2 antagonist-9	Mas-related G-protein-coupled Receptor (MRGPR)	Inflammation/Immunology
MrgprX2 antagonist-9 is an MRGPRX2 antagonist with an IC₅₀ of 0.1-100 nM. MrgprX2 antagonist-9 can be used for the research of inflammatory diseases .

HY-15705

GPR35 agonist 2	GPR35 Arrestin	Metabolic Disease Inflammation/Immunology
GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC₅₀s of 26 and 3.2 nM in the *β-arrestin* and Ca ²⁺ release assay, respectively .

HY-155480

PSB-22034	Mas-related G-protein-coupled Receptor (MRGPR)	Inflammation/Immunology
PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca ²⁺ and β-arrestin experiments, respectively .

HY-175504

MLS6357	Dopamine Receptor PERK	Neurological Disease
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .

HY-179471

PSB-17365	GPR84	Inflammation/Immunology
PSB-17365 is a potent GPR84 agonist with EC₅₀ values of 2.5 nM and 100 nM in a cAMP accumulation assay and a β-arrestin 2 recruitment assay, respectively .

HY-175505

Dopamine D3 receptor antagonist-3	Dopamine Receptor	Neurological Disease
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC₅₀ and a K_d of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .

HY-161717

MRS5663	Adenosine Receptor	Cardiovascular Disease
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 .

HY-171069

FFA2 agonist-1	Free Fatty Acid Receptor	Metabolic Disease
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 .

HY-103254R

ML221 (Standard)	Arrestin Apelin Receptor (APJ) Reference Standards	Neurological Disease
ML221 (Standard) is the analytical standard of ML221 (HY-103254). This product is intended for research and analytical applications. ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

HY-181515

KOR agonist 8	Opioid Receptor	Neurological Disease
KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a K_i value of 5.3 nM for human KOR, and EC₅₀ values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .

製品番号	製品名		Classification

HY-155480

PSB-22034		Alkynes
PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca ²⁺ and β-arrestin experiments, respectively .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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