36 Results for "

substrate channel

" in MedChemExpress (MCE) Product Catalog:
Products (36)

36 Results for "substrate channel" in MCE Product Catalog:

25
25 Publications Verification
Cat. No.: HY-B1302
CAS No.: 6151-40-2
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .
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24
24 Cited Publications
Cat. No.: HY-B1751
CAS No.: 56-54-2
Quinidine (15% dihydroquinidine) is an orally active antiarrhythmic agent. Quinidine (15% dihydroquinidine) reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine (15% dihydroquinidine) exerts sustained block and open-channel block effects on IK(f). Quinidine (15% dihydroquinidine) alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine (15% dihydroquinidine) can be used in studies related to uterine sarcoma and seizures .
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5
5 Cited Publications
Cat. No.: HY-B1793
CAS No.: 56-34-8
Target:  

Potassium Channel

Research Areas:  

Neurological Disease Cancer

Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties .
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3
3 Cited Publications
Cat. No.: HY-N6065
CAS No.: 73069-27-9
Synonyms: (+)-Praeruptorin A
Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension .
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1
1 Cited Publications
Cat. No.: HY-113037C
CAS No.: 116057-57-9
Purity:  ≥95.0%
Synonyms: Farnesyl diphosphate ammonium
Farnesyl pyrophosphate (Farnesyl diphosphate) ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases .
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1
1 Cited Publications
Cat. No.: HY-W012985
CAS No.: 600-22-6
Methyl pyruvate is a p53/p21 axis inhibitor, intrinsic apoptosis inhibitor, cytotoxic agent, ATP production enhancer, proteasome function restorer, TDP-43 localization normalizer, ATP-sensitive potassium (K +ATP) channel inhibitor, depolarizer, and insulin secretagogue .Methyl pyruvate turns off apoptotic pathways, induces cancer cell death, acts as a substrate for dimeric dihydrodiol dehydrogenase, enhances TCA cycle activity, rescues proteasome impairment and TDP-43 mislocalization, inhibits K +ATP channels independent of ATP, depolarizes pancreatic β-cell membranes, modulates insulin secretion, and enters pancreatic β-cell mitochondria via a specific transporter .Methyl pyruvate can be used for the research of lung adenocarcinoma, ovarian clear cell adenocarcinoma, breast adenocarcinoma, amyotrophic lateral sclerosis, and type II diabetes .
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1
1 Cited Publications
Cat. No.: HY-119101
CAS No.: 780750-65-4
Purity:  95.74%
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
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Cat. No.: HY-107212
CAS No.: 220119-17-5
Purity:  99.05%
Research Areas:  

Infection

Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
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Cat. No.: HY-124108
CAS No.: 1191-85-1
Purity:  ≥99.0%
Synonyms: ETYA
Eicosatetraynoic acid (ETYA) is a non-metabolizable analog of Arachidonic acid (HY-109590) and also an inhibitor of the lipoxygenase (LOX)/cyclooxygenase (COX) pathway (ID50 = 8 μM and 4 μM). Eicosatetraynoic acid acts as a suicide substrate to inhibit the production of inflammatory mediators such as leukotrienes and prostaglandins. Eicosatetraynoic acid acts directly on cell membranes and membrane proteins to exert a wide range of effects, including blocking potassium channels, increasing cell membrane fluidity, elevating intracellular calcium levels, inhibiting DNA synthesis in tumor cells, inducing differentiation of certain cells, and specifically inhibiting the assembly and replication of orthopoxviruses. Eicosatetraynoic acid alleviates acute lung injury induced by chemicals such as phosgene .
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Cat. No.: HY-136615
CAS No.: 71186-53-3
Purity:  ≥99.0%
Target:  

Potassium Channel

Research Areas:  

Neurological Disease

5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity .
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Cat. No.: HY-134136A
CAS No.: 324518-20-9
Octanoyl coenzyme A lithium is an enoyl-CoA hydratase binder. Octanoyl coenzyme A lithium binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
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Cat. No.: HY-176763
CAS No.: 2376747-46-3
Target:  

Sec61

Research Areas:  

Cancer

KZR-261 is a Sec61 translocase inhibitor. KZR-261 binds directly to the Sec61 channel, thereby inhibiting the biosynthesis of certain Sec61 substrate proteins, including oncogenic factors. KZR-261 activates the endoplasmic reticulum stress response. KZR-261 exhibits broad in vitro anticancer activity. KZR-261 shows antitumor efficacy in mouse models of cancer. KZR-261 can be used for the research of multiple myeloma, colorectal cancer, small cell lung cancer, pancreatic cancer, prostate cancer, non-Hodgkin's lymphoma, and mantle cell lymphoma .
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Cat. No.: HY-113037
CAS No.: 13058-04-3
Synonyms: (E/Z)-Farnesyl diphosphate
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
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Cat. No.: HY-132184
CAS No.: 87173-80-6
Purity:  ≥99.0%
Synonyms: 5,6-EET; (±)5,6-EpETrE
Research Areas:  

Endocrinology

5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
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Cat. No.: HY-W090942
CAS No.: 13171-93-2
Research Areas:  

Others

Z-Gly-Gly-Phe-OH is a substrate for pepsin and thermolysin. Z-Gly-Gly-Phe-OH has an IC50 of 15.8 μM for open sodium channels under pepsin catalysis. Z-Gly-Gly-Phe-OH forms peptide bonds with amine components (such as H-Leu-NHPh) through enzyme-catalyzed condensation reactions, and is active as an intermediate in peptide synthesis .
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Cat. No.: HY-N3463
CAS No.: 5835-26-7
Isopimaric acid is a coniferous tree defense compound. Isopimaric acid binds to AKT and inhibits mTOR phosphorylation, thereby regulating the AKT/mTOR pathway. Isopimaric acid inhibits oxidative stress, inflammation, microglial migration, apoptosis, autophagic flux, ornithine decarboxylase activity, breast cancer proliferation and metastasis, and fungal spore germination. Isopimaric acid also induces M2 microglial polarization, mitochondrial damage, ROS accumulation, starvation-induced colon cancer cell apoptosis, and breast cancer cell cycle arrest. Isopimaric acid activates potassium channels, regulates sodium channels and calcium channels, reduces myocardial excitability, and improves arrhythmia. Isopimaric acid acts as an oxidative substrate for CYP6BW1/3, down-regulates PINK1/Parkin, and regulates calcium homeostasis, oxidative phosphorylation, EMT, and the Wnt pathway. Isopimaric acid exhibits activity against drug-resistant Staphylococcus aureus, repels feeding, and promotes the growth of rice seedlings. Isopimaric acid is suitable for research related to epilepsy, tumors, drug-resistant bacterial infections, atrial fibrillation, hypertension, hyperlipidemia, pulmonary tuberculosis, etc .
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Cat. No.: HY-113037CS
Synonyms: Farnesyl diphosphate-d2 triammonium
Farnesyl pyrophosphate-d2 (Farnesyl diphosphate-d2) triammonium is a deuterium labeled Farnesyl pyrophosphate triammonium (HY-113037C). Farnesyl pyrophosphate ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
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Cat. No.: HY-173162
CAS No.: 86383-89-3
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
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Cat. No.: HY-113037B
CAS No.: 372-97-4
Synonyms: Farnesyl diphosphate
Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
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Cat. No.: HY-B1751D
CAS No.: 6591-63-5
Quinidine sulfate dihydrate is an orally active antiarrhythmic agent. Quinidine sulfate dihydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine sulfate dihydrate exerts sustained block and open-channel block effects on IK(f). Quinidine sulfate dihydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine sulfate dihydrate can be used in studies related to uterine sarcoma and seizures .
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