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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
767 Results for "
Competitive antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (767)
767 Results for "Competitive antagonist" in MCE Product Catalog:
73
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49 Cited Publications
Synonyms: (+)-MK 801 Maleate
Target:
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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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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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39 Cited Publications
Research Areas:
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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36 Cited Publications
Synonyms: D-APV; D-2-Amino-5-phosphonovaleric acid
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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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Research Areas:
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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Research Areas:
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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34 Cited Publications
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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34 Cited Publications
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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32 Cited Publications
Cat. No.: HY-A0013
CAS No.: 147536-97-8
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Research Areas:
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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32 Cited Publications
Cat. No.: HY-A0013A
CAS No.: 157212-55-0
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Research Areas:
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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27 Cited Publications
Synonyms: Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
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Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
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27 Cited Publications
Synonyms: Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
Target:
Research Areas:
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
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24 Cited Publications
Synonyms: AZD8797; KAND567
Research Areas:
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively .
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NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity .
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CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
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23 Cited Publications
Synonyms: FG9065 disodium
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Research Areas:
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
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23 Cited Publications
Synonyms: FG9202 disodium
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Research Areas:
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity .
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22 Cited Publications
Synonyms: (-)-Scopolamine hydrochloride; Hyoscine hydrochloride
Target:
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
