85 Results for "

receptor internalization

" in MedChemExpress (MCE) Product Catalog:
Products (85)

85 Results for "receptor internalization" in MCE Product Catalog:

10
10 Publications Verification
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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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-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-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-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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3
3 Cited Publications
Cat. No.: HY-N1166
CAS No.: 76-80-2
Synonyms: Deguelinol I; Hydroxydeguelin
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors .
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2
2 Cited Publications
Cat. No.: HY-P2259
CAS No.: 1404188-93-7
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .
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1
1 Cited Publications
Cat. No.: HY-139413
CAS No.: 9041-22-9
Purity:  99.00%
β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery . β-d-glucan is an enteric delivery vehicle for probiotics .
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1
1 Cited Publications
Cat. No.: HY-139690
CAS No.: 2615910-00-2
Purity:  98.96%
CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) .
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1
1 Cited Publications
Cat. No.: HY-P11143A
Research Areas:  

Cancer

IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1 acetate-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1 acetate-labeled liposomes accumulate more effectively within H226 tumors .
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Cat. No.: HY-175701
CAS No.: 2810808-95-6
Synonyms: RO7795081; RG6652
Target:  

Arrestin GLP Receptor

Research Areas:  

Metabolic Disease

CT-996 is an orally active GLP-1RA agonist with an EC50 of 0.49 nM. CT-996 reduces the recruitment of β-arrestin and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity .
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Cat. No.: HY-D2836
Synonyms: FITC-Hyaluronate (MW 1000000)
FITC-HA (MW 1000000) is hyaluronic acid (HA) (HY-B0633A) labeled with FITC (HY-66019). FITC-HA retains the ability of HA to bind to receptors (such as CD44) and form extracellular matrices, while it can be detected by fluorescence microscopy or flow cytometry for tracing the localization, binding, internalization and metabolic pathways of HA in cells, tissues or living organisms (Ex/Em ≈ 490/520 nM) .
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Cat. No.: HY-P99189
CAS No.: 947687-12-9
Synonyms: IMC-A12; NSC742460

Target:  

IGF-1R

Research Areas:  

Cancer

Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
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Cat. No.: HY-124071
CAS No.: 1258417-54-7
Purity:  99.96%
Research Areas:  

Inflammation/Immunology

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders .
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Cat. No.: HY-P5362
NODAGA-LM3 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC50 = 1.3 nM). NODAGA-LM3 does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. 68Ga-labeled NODAGA-LM3 can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors .
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Cat. No.: HY-P9990
CAS No.: 2407378-48-5
Synonyms: BIIB059
Litifilimab (BIIB059) is a humanized IgG1 monoclonal antibody targeting BDCA2. Litifilimab induces internalization of BDCA2 receptors on the membrane of plasmacytoid dendritic cells, inhibits the TLR7/TLR9 signaling pathway, and suppresses the production of type I interferons. Litifilimab can be used in the research of systemic and cutaneous lupus erythematosus .
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Cat. No.: HY-101265
CAS No.: 1514888-56-2
Purity:  99.90%
Synonyms: S1p receptor agonist 1
Target:  

LPL Receptor

Research Areas:  

Inflammation/Immunology

Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
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Cat. No.: HY-P3717
CAS No.: 3031514-44-7
Target:  

Ephrin Receptor

Research Areas:  

Cancer

Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines .
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Cat. No.: HY-116819
CAS No.: 1638646-27-1
Purity:  ≥98.0%
Target:  

GCGR

VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes .
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