293 Results for "

CCR3 internalization

" in MedChemExpress (MCE) Product Catalog:
Products (293)

293 Results for "CCR3 internalization" in MCE Product Catalog:

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11
11 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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11
11 Publications Verification
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 [3] .
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11
11 Publications Verification
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 [3] .
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7
7 Cited Publications
Cat. No.: HY-103363
CAS No.: 247580-43-4
Purity:  99.58%
Research Areas:  

Inflammation/Immunology Cancer

SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM. SB-328437 can inhibit eosinophil migration induced by eotaxin, eotaxin-2, and monocyte chemotactic protein-4. In addition, SB-328437 can sensitize 5-FU (HY-90006)-resistant gastric cancer cells. SB-328437 can also reduce the recruitment of neutrophils to the lungs and pulmonary inflammation during acute inflammation. SB-328437 can be used in the research of inflammation-related diseases [3].
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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-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-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-103360
CAS No.: 353791-85-2
Purity:  96.05%
Target:  

CCR

Research Areas:  

Inflammation/Immunology

J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect [3].
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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 [3] .
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4
4 Cited Publications
Cat. No.: HY-110318
CAS No.: 1785665-61-3
Purity:  98.28%
VUF11207 fumarate is a potent, selective, and orally active CXCR7/ACKR3 agonist (pKi = 8.1). VUF11207 fumarate 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 fumarate can be used for research on glioblastoma, hypertension, and venous thrombosis [3] .
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3
3 Cited Publications
Cat. No.: HY-19974
CAS No.: 333994-00-6
Target:  

CCR HIV

Research Areas:  

Infection Endocrinology

TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
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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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3
3 Cited Publications
Cat. No.: HY-141598B
CAS No.: 2238831-60-0
Synonyms: DS-1062; Dato-DXd
Datopotamab deruxtecan (DS-1062) is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
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3
3 Cited Publications
Cat. No.: HY-141598
CAS No.: 2238831-60-0
Purity:  99.54%
Synonyms: DS-1062 (solution); Dato-DXd (solution)
Research Areas:  

Cancer

Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
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3
3 Cited Publications
Cat. No.: HY-164992
Synonyms: MRG002; Trastuzumab MMAE
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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2
2 Cited Publications
Cat. No.: HY-107051
CAS No.: 408303-43-5
Purity:  98.77%
Synonyms: GW 994
Target:  

CCR

GW 766994 (GW 994) is an orally active and specific chemokine receptor-3 (CCR3) antagonist. GW 766994 has the potential for asthma and eosinophilic bronchitis research .
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2
2 Cited Publications
Cat. No.: HY-NP035
Synonyms: OVA-FITC
Ovalbumin-FITC is an ovalbumin conjugated to FITC (Ex=495 nm; Em=525 nm). Ovalbumin-FITC can be internalized by cells via endocytosis .
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