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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
9483 Results for "
competor
" in MedChemExpress (MCE) Product Catalog:
Products (9483)
9483 Results for "competor" in MCE Product Catalog:
Cat. No.: HY-118962
CAS No.: 342394-93-8
E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca 2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection .
Cat. No.: HY-136693
CAS No.: 98719-20-1
Target:
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L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
Cat. No.: HY-13749AR
CAS No.: 654671-78-0
Synonyms: MK-0431 phosphate (Standard)
Research Areas:
Sitagliptin (MK-0431) phosphate (Standard) is the analytical standard of Sitagliptin phosphate (HY-13749A). This product is intended for research and analytical applications. Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
Synonyms: MK-0431-d4 phosphate
Cat. No.: HY-13749BR
CAS No.: 654671-77-9
Synonyms: MK-0431 phosphate monohydrate (Standard)
Research Areas:
Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
Cat. No.: HY-13749R
CAS No.: 486460-32-6
Synonyms: MK-0431 (Standard)
Research Areas:
Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
Cat. No.: HY-13749S1
Purity: 99.22%
Synonyms: MK-0431-d4 hydrochloride
Cat. No.: HY-13749S2
Synonyms: MK-0431-d4
Cat. No.: HY-13749S3
CAS No.: 1133211-99-0
Synonyms: MK-0431-d6
Cat. No.: HY-187206
Target:
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CYP1B1-IN-15 is a CYP1B1 inhibitor with an IC50 of 1.47 nM, and it exhibits high selectivity against six major CYP subtypes. CYP1B1-IN-15 exerts competitive inhibitory effects by competing with substrates for binding to the active site of CYP1B1. CYP1B1-IN-15 enhances the inhibitory effect of Paclitaxel (HY-B0015) on the proliferation of paclitaxel-resistant cancer cells, and inhibits the migration and invasion of paclitaxel-resistant cancer cells. CYP1B1-IN-15 can be used in studies related to paclitaxel-resistant non-small cell lung cancer .
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MFN2 agonist-1 is an allosteric agonist of mitofusin 2 (MFN2) with an EC50 of 3 nM. MFN2 agonist-1 mimics the MFN2 HR1 peptide to compete for HR2, disrupt the HR1-HR2 autoinhibitory interaction, stabilize the open conformation of MFN2, and promote GTP hydrolysis and mitochondrial fusion. MFN2 agonist-1 acts in a manner dependent on endogenous MFN1 or MFN2, and does not impair cell viability. MFN2 agonist-1 reverses mitochondrial fragmentation, depolarization, aggregation and axonal transport defects, restores bidirectional movement and improves enhanced autophagy. MFN2 agonist-1 is used in studies related to Charcot-Marie-Tooth disease type 2A, Alzheimer's disease, Parkinson's disease and Huntington's disease .
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AM-001 is a selective Epac1 inhibitor with an IC50 value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis .
Cat. No.: HY-141466A
Purity: 97.85%
Research Areas:
Crotonyl-CoA tetrasodium, a high-energy acyl donor, is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA tetrasodium is important in the metabolism of fatty acids and amino acids. Crotonyl-CoA tetrasodium acts as a substrate for p300’s histone crotonyltransferase activity, competing with acetyl-CoA for p300-mediated histone acylation reactions. Crotonyl-CoA tetrasodium regulates global and gene-specific histone crotonylation levels in cells, with cellular concentration changes altering histone crotonylation at regulatory elements of activated genes. Crotonyl-CoA tetrasodium serves as the substrate for crotonyl-CoA reductase/carboxylase (CCRC)-catalyzed NADPH-mediated reduction and carbon dioxide trapping to form unusual alkylmalonyl-CoA polyketide synthase extender units. Crotonyl-CoA tetrasodium can be used for the research of LPS-induced inflammatory response .
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GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
Cat. No.: HY-148611
CAS No.: 1135037-53-4
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NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases .
Cat. No.: HY-166309
CAS No.: 116912-55-1
Research Areas:
Crotonyl-CoA tetralithium, a high-energy acyl donor, is an intermediate in the fermentation of butyric acid, and in the metabolism of lysine and tryptophan. Crotonyl-CoA tetralithium is important in the metabolism of fatty acids and amino acids. Crotonyl-CoA tetralithium acts as a substrate for p300’s histone crotonyltransferase activity, competing with acetyl-CoA for p300-mediated histone acylation reactions. Crotonyl-CoA tetralithium regulates global and gene-specific histone crotonylation levels in cells, with cellular concentration changes altering histone crotonylation at regulatory elements of activated genes. Crotonyl-CoA tetralithium serves as the substrate for crotonyl-CoA reductase/carboxylase (CCRC)-catalyzed NADPH-mediated reduction and carbon dioxide trapping to form unusual alkylmalonyl-CoA polyketide synthase extender units. Crotonyl-CoA tetralithium can be used for the research of LPS-induced inflammatory response .
Cat. No.: HY-W035399S
Cat. No.: HY-W035399S1
CAS No.: 2708340-91-2
Cat. No.: HY-Y1804S
CAS No.: 2714413-18-8
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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
