Search Result

Pathways Recommended:	GPCR/G Protein

Results for "

G protein bias

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Angiotensin Receptor (4) Apelin Receptor (APJ) (1) Arrestin (2) Cannabinoid Receptor (1) CXCR (2) Dopamine Receptor (2) G protein-coupled Bile Acid Receptor 1 (2) GPR84 (2) LPL Receptor (1) Neurotensin Receptor (2) Opioid Receptor (5)
By Research Areas:	Cancer (3) Cardiovascular Disease (6) Endocrinology (2) Inflammation/Immunology (4) Neurological Disease (13)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103080

CMF019	Apelin Receptor (APJ)	Cardiovascular Disease
CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .

HY-P3136

TRV055 TRV120055	Angiotensin Receptor	Cardiovascular Disease
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling .

HY-P3136A

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 hydrochloride, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 hydrochloride is efficacious in stimulating cellular Gq-mediated signaling .

HY-19863

F-15599 2 Publications Verification NLX-101	5-HT Receptor	Neurological Disease
F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

HY-141495

(Rac)-Razpipadon 1 Publications Verification PW0464	Dopamine Receptor	Neurological Disease
PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC₅₀ of 5.8 nM (Gs-cAMP) .

HY-16642A

LY2828360	Cannabinoid Receptor	Neurological Disease
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB₂) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

HY-19863A

F-15599 tosylate NLX-101 tosylate	5-HT Receptor	Neurological Disease
F-15599 tosylate is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

HY-139677

5-HT7R antagonist 1	G protein-coupled Bile Acid Receptor 1	Neurological Disease
5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT₇R (K_i = 6.5 nM).

HY-163917

SalA-VS-08	Opioid Receptor	Neurological Disease
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .

HY-161812

MOR agonist-4	Opioid Receptor	Others
MOR agonist-4 (2d) is a G protein signaling-biased Kappa opioid receptor (KOR) agonist with an EC₅₀ value of 11 nM. MOR agonist-4 contains an electron withdrawing CF3 group and a bias factor of 38 based on triazole. MOR agonist-4 is used in the research of pruritis and analgesia .

HY-139677A

5-HT7R antagonist 1 free base	G protein-coupled Bile Acid Receptor 1	Neurological Disease
5-HT7R antagonist 1 (free base) is a G protein-biased antagonist against 5-HT₇R (K_i = 6.5 nM).

HY-163916

SalA-VS-07	Opioid Receptor	Neurological Disease
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .

HY-161106

OX04528	GPR84	Inflammation/Immunology Cancer
OX04528 (compound 68) is a potent, G-protein biased, and orally active GPR84 agonist. OX04528 no cytotoxicity. OX04528 inhibits cAMP production with an EC₅₀ value of 0.00598 nM .

HY-161107

OX04529	GPR84	Inflammation/Immunology
OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC₅₀ of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .

HY-164795

SBI-810	Neurotensin Receptor	Neurological Disease
SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .

HY-164795A

SBI-810 hydrochloride	Neurotensin Receptor	Neurological Disease
SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
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 .

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-159923

BPRMU191	Opioid Receptor	Neurological Disease
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .

HY-P0172A

ATI-2341 TFA 2 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P0172

ATI-2341	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P2141A

TRV-120027 TFA 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027 TFA, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .

HY-P2141

TRV-120027 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the?acute decompensated heart failure (ADHF) treatment .

HY-115831

SAR247799 S1P1 agonist 3	LPL Receptor	Cardiovascular Disease
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC₅₀s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .

Cat. No.	Product Name	Target	Research Area

HY-P3136

TRV055 TRV120055	Angiotensin Receptor	Cardiovascular Disease
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling .

HY-P3136A

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 hydrochloride, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 hydrochloride is efficacious in stimulating cellular Gq-mediated signaling .

HY-P0172A

ATI-2341 TFA 2 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P2141A

TRV-120027 TFA 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027 TFA, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .

HY-P2141

TRV-120027 3 Publications Verification	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the?acute decompensated heart failure (ADHF) treatment .

HY-P0172

ATI-2341	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

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