421 Results for "

GPCR internalization

" in MedChemExpress (MCE) Product Catalog:
Products (421)

421 Results for "GPCR internalization" in MCE Product Catalog:

266
266 Publications Verification
Cat. No.: HY-13948
CAS No.: 4474-91-3
Purity:  99.98%
Synonyms: Angiotensin II; Ang II; DRVYIHPF
Angiotensin II (Angiotensin II) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .
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266
266 Publications Verification
Cat. No.: HY-13948A
CAS No.: 68521-88-0
Purity:  99.62%
Synonyms: Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate
Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .
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266
266 Publications Verification
Cat. No.: HY-13948B
CAS No.: 2761969-44-0
Purity:  98.84%
Synonyms: Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA
Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .
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42
42 Cited Publications
Cat. No.: HY-111534
CAS No.: 882366-16-7
Purity:  99.22%
Research Areas:  

Others

SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5 .
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33
33 Cited Publications
Cat. No.: HY-13771A
CAS No.: 2898-95-5
Purity:  99.06%
Synonyms: Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .
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33
33 Cited Publications
Cat. No.: HY-13771
CAS No.: 128-13-2
Purity:  99.94%
Synonyms: Ursodeoxycholate; Ursodiol; UDCA
Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active .
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11
11 Cited Publications
Cat. No.: HY-W008947
CAS No.: 256414-75-2
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .
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11
11 Cited Publications
Cat. No.: HY-12355
CAS No.: 1230487-00-9
Purity:  99.95%
Synonyms: BAF-312
Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis .
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11
11 Cited Publications
Cat. No.: HY-12355A
CAS No.: 1234627-85-0
Purity:  99.64%
Synonyms: BAF-312 hemifumarate
Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis .
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9
9 Cited Publications
Cat. No.: HY-15589
CAS No.: 885101-89-3
Purity:  99.23%
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
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7
7 Cited Publications
Cat. No.: HY-N0169
CAS No.: 83-49-8
Synonyms: HDCA
Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
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7
7 Cited Publications
Cat. No.: HY-N0169A
CAS No.: 10421-49-5
Synonyms: HDCA sodium
Hyodeoxycholic acid sodium is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells .
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7
7 Cited Publications
Cat. No.: HY-113962
CAS No.: 64907-22-8
Purity:  99.88%
Synonyms: 7α,25-OHC
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
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6
6 Cited Publications
Cat. No.: HY-111793A
CAS No.: 2749281-71-6
Purity:  98.19%
Target:  

CXCR

Research Areas:  

Neurological Disease

NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo .
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6
6 Cited Publications
Cat. No.: HY-111793
CAS No.: 1060524-97-1
Purity:  98.40%
Target:  

CXCR

Research Areas:  

Neurological Disease

NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo .
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6
6 Cited Publications
Cat. No.: HY-P2106
CAS No.: 1886973-05-2
Research Areas:  

Cardiovascular Disease

Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
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6
6 Cited Publications
Cat. No.: HY-P2106A
Research Areas:  

Cardiovascular Disease

Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
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4
4 Cited Publications
Cat. No.: HY-W010907
CAS No.: 6640-22-8
Target:  

GPR35 ERK

Research Areas:  

Neurological Disease

Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
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4
4 Cited Publications
Cat. No.: HY-P2336A
Target:  

Melanocortin Receptor

Research Areas:  

Cancer

CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
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4
4 Cited Publications
Cat. No.: HY-100677
CAS No.: 1378524-41-4
Purity:  94.56%
VUF11207 is a potent, selective, and orally active CXCR7/ACKR3 agonist (pKi = 8.1). VUF11207 specifically activates CXCR7/ACKR3, recruits β-arrestin, and induces receptor internalization, while downregulating the pro-inflammatory, pro-osteoclastogenic, and tumor immunosuppressive signaling mediated by the CXCL12-CXCR4 axis. VUF11207 can be used for research on glioblastoma, hypertension, and venous thrombosis .
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