Search Result

Pathways Recommended:	Neuronal Signaling JAK/STAT Signaling

Results for "

Gq signaling

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (6) Adhesion G Protein-coupled Receptors (AGPCRs) (1) Adrenergic Receptor (1) Akt (1) Amyloid-β (1) Angiotensin Receptor (1) Arrestin (3) Cholecystokinin Receptor (2) Cholinesterase (ChE) (1) Drug Derivative (1) ERK (3) Free Fatty Acid Receptor (1) GHSR (1) GLP Receptor (1) GSK-3 (1) iGluR (2) Leukotriene Receptor (1) mAChR (3) MMP (1) Neurotensin Receptor (2) PACAP Receptor (1) PI3K (1) PKA (1) Protease Activated Receptor (PAR) (1) Reference Standards (1) Serotonin Transporter (1) Sodium Channel (2) Trace Amine-associated Receptor (TAAR) (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (15)

By Targets:

5-HT Receptor (6)

Adhesion G Protein-coupled Receptors (AGPCRs) (1)

Adrenergic Receptor (1)

Akt (1)

Amyloid-β (1)

Angiotensin Receptor (1)

Arrestin (3)

Cholecystokinin Receptor (2)

Cholinesterase (ChE) (1)

Drug Derivative (1)

ERK (3)

Free Fatty Acid Receptor (1)

GHSR (1)

GLP Receptor (1)

GSK-3 (1)

iGluR (2)

Leukotriene Receptor (1)

mAChR (3)

MMP (1)

Neurotensin Receptor (2)

PACAP Receptor (1)

PI3K (1)

PKA (1)

Protease Activated Receptor (PAR) (1)

Reference Standards (1)

Serotonin Transporter (1)

Sodium Channel (2)

Trace Amine-associated Receptor (TAAR) (1)

By Research Areas:

Cancer (2)

Cardiovascular Disease (1)

Inflammation/Immunology (1)

Metabolic Disease (2)

Neurological Disease (15)

Inhibitors & Agonists

Peptides

Targets Recommended: RGS Protein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P3137

TRV056	Angiotensin Receptor	Cardiovascular Disease
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .

HY-107111

GSK1034702	mAChR	Neurological Disease
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the *Gq/11* protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-169841

IHCH-7086	5-HT Receptor Arrestin	Neurological Disease
IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT_2AR with a K_i of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression .

HY-164795

SBI-810	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .

HY-164795A

SBI-810 hydrochloride	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .

HY-P6292

KS-133	PACAP Receptor PKA ERK PI3K Akt GSK-3	Neurological Disease Cancer
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .

HY-42346

ZH8651	Trace Amine-associated Receptor (TAAR)	Neurological Disease
ZH8651 is an agonist of TAAR1 which can activate both Gs and Gq signal pathway. ZH8651 can used in study schizophrenia .

HY-P10365

VPM-p15	Adhesion G Protein-coupled Receptors (AGPCRs)	Others
Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members .

HY-176921

ONO-2570366	Leukotriene Receptor	Inflammation/Immunology
ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC₅₀ = 14 nM). ONO-2570366 inhibits the binding of LTD₄Gq signaling pathway mediated by receptor activation. ONO-2570366 can be used for the researches of inflammation and immunology, such as asthma .

HY-P5358

YFLLRNP	Protease Activated Receptor (PAR)	Others
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))

HY-175515

5-HT2C agonist-11	5-HT Receptor	Neurological Disease
5-HT2C agonist-11 (Compound 1) is an orally active, brain-penetrant and selective 5-HT_2C receptor agonist (EC₅₀=15 nM). 5-HT2C agonist-11 activates the Gq protein signaling pathway, promoting intracellular calcium release. 5-HT2C agonist-11 is promising for research of depression, post-traumatic stress disorder (PTSD) and neuropathic pain .

HY-P11540

CCKBR agonist-1	Cholecystokinin Receptor MMP Amyloid-β	Neurological Disease
CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC₅₀ of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC₅₀ of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease .

HY-156532C

(-)-5-HT2C agonist-3	5-HT Receptor	Neurological Disease
(-)-5-HT2C agonist-3 (compound (-)-19) is a 5-HT_2C selective agonist with G_q signaling preference, with EC₅₀ values for 5-HT₂ receptors of 5-HT_2C: 103 nM; 5-HT_2B: 570 nM; 5-HT_2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .

HY-121140

AZ1729	Free Fatty Acid Receptor	Metabolic Disease
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in G_i-mediated pathways, but not at those transduced by G_q/G₁₁. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .

HY-107111A

GSK1034702 hydrochloride	Cholinesterase (ChE) mAChR	Neurological Disease
GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the *Gq/11* protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-P1432A

K-(D-1-Nal)-FwLL-NH2 TFA	GHSR	Cancer
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (K_i values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

HY-181878

Z8779877149 Z7149	Serotonin Transporter Adrenergic Receptor 5-HT Receptor	Neurological Disease
Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (K_i=198 nM), α2A adrenergic receptor (K_i=180 nM; EC₅₀=440 nM) and 5-HT_2A receptor (EC₅₀=172 nM, E_max=76%). Z8779877149 inhibits 5-HT reuptake and activates G_i and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .

HY-145156

CHU-128	GLP Receptor	Metabolic Disease
CHU-128 is an effective and selective GLP-1R agonist. CHU-128 exhibits strong signal specificity and can activate the Gs/cAMP pathway, but it cannot activate the Gq/calcium signal, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 can be used for research on type 2 diabetes .

HY-179721

CCKBR agonist-2	Cholecystokinin Receptor	Neurological Disease
CCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway (EC₅₀ = 0.27 nM), but has almost no activity on Gq and Gs signaling pathways. CCKBR agonist-2 shows no significant protective effect in the mouse Alzheimer's disease model, proving that the simple activation of the Gi signal pathway does not play a dominant role in the improvement of cognitive function .

HY-107111R

GSK1034702 (Standard)	Reference Standards mAChR	Neurological Disease
GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-186169

R-MDDMA	5-HT Receptor Drug Derivative	Neurological Disease
R-MDDMA, 4-methylenedioxymethamphetamine (MDMA) analogue, is a 5-HT2A/5-HT2C receptor modulator. R-MDDMA shows antagonistic activity against 5-HT2A/5-HT2C with IC₅₀ values of 642 and 137 nM, and also shows partial agonist activity with EC₅₀ values of 24.5 and 14.4 nM, but does not activate 5-HT2B receptors. R-MDDMA promotes cortical neuron growth. R-MDDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDDMA can be used for the researches of post-traumatic stress disorder and depression .

HY-186170

R-MDMA	5-HT Receptor	Neurological Disease
R-MDMA, 4-methylenedioxymethamphetamine (MDMA) isomer, is a 5-HT2A/5-HT2C receptor antagonist with an IC₅₀ of 629 and 61.4 nM. R-MDMA promotes cortical neuron growth. R-MDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDMA can be used for the researches of post-traumatic stress disorder and depression .

Cat. No.	Product Name	Target	Research Area