825 Results for "

Competitive antagonist

" in MedChemExpress (MCE) Product Catalog:
Products (825)

825 Results for "Competitive antagonist" in MCE Product Catalog:

80
Colchicine
Colchicine
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80 Publications Verification
Cat. No.: HY-16569
CAS No.: 64-86-8
Category:  

Natural Products Plants Other Families Extract Disease Research Fields Cancer

Target:  

Environmental Pollutants Apoptosis Autophagy Microtubule/Tubulin NOD-like Receptor (NLR)

Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
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53
Dizocilpine maleate
Dizocilpine maleate
0 Images
53 Cited Publications
Cat. No.: HY-15084
CAS No.: 77086-22-7
Purity:  99.99%
Synonyms: (+)-MK 801 Maleate
Target:  

iGluR

Research Areas:  

Neurological Disease

Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
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53
Dizocilpine
Dizocilpine
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53 Cited Publications
Cat. No.: HY-15084B
CAS No.: 77086-21-6
Purity:  99.90%
Synonyms: MK-801
Target:  

iGluR

Research Areas:  

Neurological Disease

Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
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46
Exendin(9-39) amide
Exendin(9-39) amide
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46 Cited Publications
Cat. No.: HY-P0264
CAS No.: 133514-43-9
Synonyms: Avexitide
Target:  

GLP Receptor

Exendin (9-39) amide (Avexitide) is a competitive GLP-1R antagonist. Exendin (9-39) amide blocks the Semaglutide (HY-114118)-induced increase in insulin secretion and also attenuates the hypoglycemic effect of Semaglutide. Exendin (9-39) amide abolishes the islet-protective effect of Liraglutide. Exendin (9-39) amide can be used in research on type 2 diabetes and type 1 diabetes .
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46
Exendin(9-39) amide acetate
Exendin(9-39) amide acetate
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46 Cited Publications
Cat. No.: HY-P0264A
CAS No.: 2051593-46-3
Synonyms: Avexitide acetate
Target:  

GLP Receptor

Research Areas:  

Metabolic Disease Inflammation/Immunology

Exendin (9-39) amide acetate (Avexitide acetate) is a competitive GLP-1R antagonist. Exendin (9-39) amide acetate blocks the Semaglutide (HY-114118)-induced increase in insulin secretion and also attenuates the hypoglycemic effect of Semaglutide. Exendin (9-39) amide acetate abolishes the islet-protective effect of Liraglutide. Exendin (9-39) amide acetate can be used in research on type 2 diabetes and type 1 diabetes .
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43
ANA-12
ANA-12
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43 Cited Publications
Cat. No.: HY-12497
CAS No.: 219766-25-3
Purity:  99.90%
Target:  

Trk Receptor NOD-like Receptor (NLR) AIM2 Caspase

Research Areas:  

Neurological Disease Inflammation/Immunology

ANA-12 is a brain-penetrant, selective TrkB antagonist with IC50 values of 45.6 nM and 41.1 μM, and Kd values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory .
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41
D-AP5
D-AP5
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41 Cited Publications
Cat. No.: HY-100714A
CAS No.: 79055-68-8
Purity:  99.94%
Synonyms: D-APV; D-2-Amino-5-phosphonovaleric acid
Target:  

iGluR

Research Areas:  

Neurological Disease

D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
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40
MK-571
MK-571
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40 Cited Publications
Cat. No.: HY-19989
CAS No.: 115104-28-4
Synonyms: L-660711
Target:  

P-glycoprotein LPL Receptor Leukotriene Receptor

Research Areas:  

Inflammation/Immunology

MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
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40
MK-571 sodium
MK-571 sodium
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40 Cited Publications
Cat. No.: HY-19989A
CAS No.: 115103-85-0
Synonyms: L-660711 sodium
Target:  

P-glycoprotein LPL Receptor Leukotriene Receptor

Research Areas:  

Inflammation/Immunology

MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
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36
V-9302
V-9302
0 Images
36 Cited Publications
Cat. No.: HY-112683
CAS No.: 1855871-76-9
Purity:  99.88%
Target:  

ASCT

Research Areas:  

Cancer

V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells .
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36
V-9302 hydrochloride
V-9302 hydrochloride
0 Images
36 Cited Publications
Cat. No.: HY-112683A
CAS No.: 2416138-42-4
Purity:  99.10%
Target:  

ASCT

Research Areas:  

Cancer

V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
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33
Bosentan
Bosentan
0 Images
33 Cited Publications
Cat. No.: HY-A0013
CAS No.: 147536-97-8
Target:  

Endothelin Receptor

Research Areas:  

Cardiovascular Disease Endocrinology Cancer

Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
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33
Bosentan hydrate
Bosentan hydrate
0 Images
33 Cited Publications
Cat. No.: HY-A0013A
CAS No.: 157212-55-0
Target:  

Endothelin Receptor

Research Areas:  

Cardiovascular Disease Endocrinology Cancer

Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
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29
Atropine
Atropine
0 Images
29 Cited Publications
Cat. No.: HY-B1205
CAS No.: 51-55-8
Synonyms: Tropine tropate; DL-Hyoscyamine
Category:  

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