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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
232 Results for "
efflux inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (232)
232 Results for "efflux inhibitor" in MCE Product Catalog:
50
Research Areas:
Methyllycaconitine (MLA) citrate is a blood-brain barrier-permeable antagonist of α7 nicotinic acetylcholine receptor (α7nAChR) with an IC50 of 2 nM. Methyllycaconitine citrate inhibits Aβ25-35-induced autophagy by restoring the mTOR pathway, and prevents reactive oxygen species (ROS) production, microglial activation, reduced dopamine uptake, loss of dopaminergic terminals and catecholamine secretion. Methyllycaconitine citrate induces hippocampal glutamate efflux, enhances long-term potentiation, and improves memory acquisition. Methyllycaconitine citrate can be used in research related to Alzheimer's disease, cerebral palsy, Parkinson's disease and schizophrenia .
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31 Cited Publications
Cat. No.: HY-50879
CAS No.: 143664-11-3
Synonyms: GF120918; GW0918; GG918; GW120918
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Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
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Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .
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18
18 Cited Publications
Cat. No.: HY-B0193A
CAS No.: 19237-84-4
Target:
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Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
13
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Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
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12 Cited Publications
Synonyms: MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride
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10 Cited Publications
Synonyms: ML-SI3 (cis/trans mix)
Target:
Research Areas:
ML-SI3 is a mixture of cis/trans ML-SI3 (HY-139426A), which is a TRPML1/2 channel inhibitor with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy. The cis/trans ML-SI3 (HY-139426A) components of ML-SI3 are TRPML2 activators with EC50s of 3.3 μM and 9.4 μM, respectively .
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9 Cited Publications
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Research Areas:
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
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6 Cited Publications
Cat. No.: HY-112220
CAS No.: 2095668-10-1
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VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia .
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Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases .
5
Category:
Infection Flavonoids Flavones Plants Compositae Disease Research Fields Genista maderensis (Webb & Berthel.) Lowe Inflammation/Immunology
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4
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Pinacidil (P-1134) is a potent activator of ATP-sensitive potassium channel. Pinacidil is an antihypertensive agent hyperpolarizes vascular smooth muscle by opening K + channels. Pinacidil enhances K +-efflux in smooth muscle. Pinacidil has vasorelaxant properties. Pinacidil is able to inhibit spontaneous tone and of reducing agonist induced contractions. Pinacidil can be studied in research area such as cardiovascular diseases .
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4 Cited Publications
Synonyms: P-1134 monohydrate
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Research Areas:
Pinacidil (P-1134) monohydrate is a potent activator of ATP-sensitive potassium channel. Pinacidil monohydrate is an antihypertensive agent hyperpolarizes vascular smooth muscle by opening K + channels. Pinacidil monohydrate enhances K +-efflux in smooth muscle. Pinacidil monohydrate has vasorelaxant properties. Pinacidil monohydrate is able to inhibit spontaneous tone and of reducing agonist induced contractions. Pinacidil monohydrate can be studied in research area such as cardiovascular diseases .
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4
Category:
4
4 Cited Publications
Cat. No.: HY-N1423B
CAS No.: 1192657-83-2
3
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Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .
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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
