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GTPγS assays

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By Targets:	5-HT Receptor (2) Cannabinoid Receptor (1) GPR88 (2) Transmembrane Glycoprotein (1)
By Research Areas:	Metabolic Disease (1) Neurological Disease (5)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-167856

RTI-122	GPR88	Neurological Disease
RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC₅₀=11 nM), with EC₅₀ values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ ³⁵S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T_1/2=5.8 h) and can be used to investigate alcohol use disorder .

HY-128111

ASN02563583	Transmembrane Glycoprotein	Neurological Disease
ASN02563583, a compound that regulates the activity of the GPR17 receptor, has a IC₅₀ value of 0.64 nM in [₃₅S]GTPγS binding assay. ASN02563583 can be used in the study of neurological diseases .

HY-114678

LY302148	5-HT Receptor	Neurological Disease
LY302148 is a receptor ligand for 5-HT_1F. Compared to the E_max of 5-HT, LY302148 behaves as a partial agonist for the 5-HT_1F receptor. In the [ ³⁵S]GTPγS binding assay targeting human 5-HT_1F receptors, LY302148 exhibits good potency with an EC₅₀ value of 5.23 nM. LY302148 can be used in the research of migraine .

HY-116065

CUMI-101	5-HT Receptor	Neurological Disease
CUMI-101 (compound 8) is a 5-HT_1AR agonist (K_i=0.15 nM) with an EC₅₀ of 0.1 nM in the [35S]GTPγS binding assay. CUMI-101 can be used in the research of neurological diseases .

HY-182697

RTICBM-74	Cannabinoid Receptor	Metabolic Disease
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC₅₀ values of 23 nM (calcium mobilization assay) and 153 nM ([ ³⁵S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .

HY-167856A

RTI-122 dihydrochloride	GPR88	Neurological Disease
RTI-122 dihydrochloride is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC₅₀=11 nM), with EC₅₀ values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ ³⁵S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride exhibits metabolic stability in mice (T_1/2=5.8 h) and can be used to investigate alcohol use disorder .

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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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GTPγS assays

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