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orthosteric+agonist

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By Targets:	Adrenergic Receptor (1) Apoptosis (2) Arrestin (1) Cannabinoid Receptor (1) Endogenous Metabolite (2) Free Fatty Acid Receptor (2) GPR84 (1) Hydroxycarboxylic Acid Receptor (HCAR) (1) mAChR (1) Mas-related G-protein-coupled Receptor (MRGPR) (1) mGluR (4) Opioid Receptor (1) PERK (1) Prostaglandin Receptor (1) Reference Standards (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (6)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W011417

Cinnabarinic acid 1 Publications Verification	Endogenous Metabolite mGluR Apoptosis	Others
Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .

HY-120645

BMS-986122 1 Publications Verification	Opioid Receptor	Neurological Disease
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ ³⁵S]GTPγS binding in mouse brain membranes .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-W011417R

Cinnabarinic acid (Standard)	Endogenous Metabolite Reference Standards mGluR Apoptosis	Others
Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .

HY-117764

LSP4-2022	mGluR	Neurological Disease
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC₅₀ of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .

HY-156025

*HCAR2 agonist* 1**	Hydroxycarboxylic Acid Receptor (HCAR)	Inflammation/Immunology
HCAR2 agonist 1 (Compound 9n) is a G_i protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the G_i protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .

HY-59384

MOMBA	Free Fatty Acid Receptor	Metabolic Disease Inflammation/Immunology
MOMBA is a selective FFA2 (Free Fatty Acid Receptor 2) orthosteric agonist that activates receptor signaling pathways by binding to the orthosteric site of FFA2 with high specificity. MOMBA holds potential for research on metabolic and inflammatory diseases .

HY-103549

Z-Cyclopentyl-AP4	mGluR	Neurological Disease
Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .

HY-142972

19(S)-HETE	Prostaglandin Receptor	Cardiovascular Disease
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC₅₀ value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .

HY-175672

MRGPRX4 modulator-3	Mas-related G-protein-coupled Receptor (MRGPR)	Neurological Disease
MRGPRX4 modulator-3 (Compound 1C) is a negative allosteric MAS-related G-protein-coupled receptor X4 (MRGPRX4) modulator. MRGPRX4 modulator-3 significantly attenuates Nateglinide (HY-B0422) (orthosteric agonist)-induced responses with an IC₅₀ of 337 nM. MRGPRX4 modulator-3 can be used for chronic itch (especially cholestatic itch) and pain research .

HY-182723

PSB-16671	GPR84	Cancer
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 .

HY-182729

*FFA2 agonist-2*	Free Fatty Acid Receptor	Metabolic Disease
FFA2 agonist-2 is a potent agonist of the FFA2 (GPR43) receptor, with a pEC₅₀ of 7.9 for human FFA2, and a pEC₅₀ of 7.3 for murine FFA2. FFA2 agonist-2 acts as an orthosteric agonist and shows no obvious cross‑activity against FFA1, FFA3 and FFA4. FFA2 agonist-2 can be used for FFA2 receptor research in type 2 diabetes and metabolic disorders .

HY-120093

GAT100	Cannabinoid Receptor PERK	Neurological Disease
GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases .

HY-121837

β2AR-IN-15	Adrenergic Receptor Arrestin	Cardiovascular Disease Inflammation/Immunology
β2AR-IN-15 is a selective β2-adrenergic receptor (β2AR) antagonist with a K_d of 1.7 μM. β2AR-IN-15 binds to an intracellular β2AR region overlapping the G-protein binding site, enhancing orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists with EC₅₀ values of 1.9 and 0.48 μM. β2AR-IN-15 shows inhibitory effect on cAMP production and β-arrestin recruitment to activated β2AR. β2AR-IN-15 can be used for the research of cardiovascular and pulmonary diseases .

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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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orthosteric+agonist

Inhibitors & Agonists