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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
105 Results for "
inward
" in MedChemExpress (MCE) Product Catalog:
Products (105)
105 Results for "inward" in MCE Product Catalog:
34
34 Publications Verification
Cat. No.: HY-19545A
CAS No.: 125941-87-9
Synonyms: R-(+)-SCH-23390 hydrochloride
Research Areas:
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
11
11 Cited Publications
Synonyms: NP-120; RC-61-91
Research Areas:
Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
11
11 Cited Publications
Synonyms: NP-120 tartrate; RC-61-91 tartrate
7
7 Cited Publications
Target:
Research Areas:
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
7
7 Cited Publications
Cat. No.: HY-A0170
CAS No.: 147059-72-1
Target:
Research Areas:
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
5
Target:
Research Areas:
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
5
5 Cited Publications
Cat. No.: HY-17401
CAS No.: 95635-56-6
Synonyms: CVT 303 dihydrochloride; RS 43285
Target:
Research Areas:
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor .
3
3
3 Cited Publications
Target:
Research Areas:
VU590 is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 is not a good probe of ROMK function in the kidney .
3
3 Cited Publications
Cat. No.: HY-114633
CAS No.: 901008-62-6
Target:
Research Areas:
VU625 is an inhibitor for potassium channel, that selectively inhibits mosquito Aedes aegypti inward rectifier potassium channel 1 (AeKir), with IC50 of 96.8 nM in HEK293 cell. VU625 can be used in development of insecticide .
2
Target:
Research Areas:
Tolazamide (U-17835) is an orally active sulfonylurea agent that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). Tolazamide has anti-diabetic properties. Tolazamide can lower blood glucose in sulfonylurea class. Tolazamide decreases insulin dose while continuing to maintain adequate metabolic control. Tolazamide is able to improve or normalize hyperglycemia and HbA .
2
2 Cited Publications
Synonyms: Dicorantil; SC-7031
Target:
Research Areas:
Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action .
2
2 Cited Publications
Synonyms: Dicorantil phosphate; SC-7031 phosphate
Target:
Research Areas:
Disopyramide phosphate is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action .
2
2 Cited Publications
Synonyms: UL-FS-49; UL-FS-49CL
Target:
Research Areas:
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
2
2 Cited Publications
Synonyms: UL-FS-49 free base; UL-FS-49CL free base
Target:
Research Areas:
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
1
Target:
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Flupirtine (D 9998) is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
1
1 Cited Publications
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
1
1 Cited Publications
Target:
Research Areas:
Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
1
1 Cited Publications
Synonyms: 2-Guanidine-4-methylquinazoline hydrochloride
Target:
Research Areas:
GMQ (hydrochloride) is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ (hydrochloride) opens only ASIC3 but no other ASICs at pH 7.4. GMQ (hydrochloride) can be used for neurological disease research .
1
1 Cited Publications
Target:
Research Areas:
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration .
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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
