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Pathways Recommended:	GPCR/G Protein

Results for "

Gαq

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Angiotensin Receptor (3) Apoptosis (2) Calcium Channel (1) ERK (3) GPR84 (1) Liposome (1) P2Y Receptor (1) PKC (1) Protease Activated Receptor (PAR) (2) Trace Amine-associated Receptor (TAAR) (1) TSH Receptor (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (6) Endocrinology (2) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (2)
Oligonucleotides:	Phospholipids (1)

14

Inhibitors & Agonists

3

Peptides

2

Natural
Products

1

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

YM-254890 10+ Cited Publications	P2Y Receptor	Cardiovascular Disease
YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y₁ signal transduction pathway, with an IC₅₀ value below 0.6 μM .

[Val4] Angiotensin III	Angiotensin Receptor	Cardiovascular Disease
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gα_q and βarr2 response, with pEC₅₀ values of 8.31 and 8.44, respectively .

FR900359	Apoptosis ERK	Cardiovascular Disease Cancer
FR900359 is a depsipeptide selective inhibitor of Gα_q/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .

MS437	TSH Receptor	Endocrinology
MS437 is a potent TSH receptor (TSHR) stimulator with an EC₅₀ value of 13x10 ^-8M. MS437 shows potent activation of G_sα, Gαq and Gα₁₂ and up-regulation of thyroglobulin (Tg), sodium iodine symporter (NIS) and TSHR gene expressions .

POPG sodium salt PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)	Liposome	Neurological Disease
POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ₁γ₁ for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .

I-287	Protease Activated Receptor (PAR) ERK	Inflammation/Immunology
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gα_q and Gα_12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research .

Gαq/11 protein-IN-1	Trace Amine-associated Receptor (TAAR)	Cancer
Gαq/11 protein-IN-1 (compound F33) is an inhibitor of Gαq/11 protein with an IC₅₀ value of 9.4 μM. Gαq/11 protein-IN-1 has antitumor activity .

WU-07047	Calcium Channel	Cardiovascular Disease
WU-07047, a simplified analog of YM-254890 (HY-111557), is a selective Gαq/11 inhibitor. WU-07047 can inhibit nucleotide exchange .

Q94 hydrochloride	Protease Activated Receptor (PAR)	Others
Q94 hydrochloride, a selective PAR₁ antagonist (IC₅₀=916 nM), can selectively block *PAR₁/Gαq interaction and signalling. Q94 hydrochloride blocks PAR₁-mediated increases in both CCL2* mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .

GPR84 agonist-2	GPR84	Inflammation/Immunology
GPR84 agonist-2 (Compound 8e) is a highly selective GPR84 agonist with an EC₅₀ value of 7.24 nM. GPR84 agonist-2 activates the Gαq signaling pathway, promoting inositol trisphosphate (IP3) production and calcium release and enhancing neutrophil chemotaxis and pro-inflammatory cytokine release. GPR84 agonist-2 is promising for research of inflammatory diseases, such as ulcerative colitis and acute lung injury .

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 (TRV120055) (hydrochloride) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

Thyrotropin 1 Publications Verification TSH; Pretiron	TSH Receptor PKC Apoptosis	Metabolic Disease Inflammation/Immunology Endocrinology Cancer
Thyrotropin (TSH, Pretiron) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin prevents Apoptosis. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism .

S 32212 hydrochloride	5-HT Receptor	Neurological Disease
S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC₅₀=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.

Cat. No.	Product Name	Target	Research Area

[Val4] Angiotensin III	Angiotensin Receptor	Cardiovascular Disease
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gα_q and βarr2 response, with pEC₅₀ values of 8.31 and 8.44, respectively .

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 (TRV120055) (hydrochloride) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

Cat. No.	Product Name		Classification

POPG sodium salt PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)		Phospholipids
POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ₁γ₁ for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .

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