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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
229 Results for "
Kv
" in MedChemExpress (MCE) Product Catalog:
Products (229)
229 Results for "Kv" in MCE Product Catalog:
22
22
Research Areas:
Infection Cardiovascular Disease Inflammation/Immunology Cancer
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
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22 Publications Verification
Cat. No.: HY-N1584A
CAS No.: 64924-67-0
Synonyms: RU-19110 hydrobromide
20
Research Areas:
Infection Cardiovascular Disease Inflammation/Immunology Cancer
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
13
13 Cited Publications
Synonyms: 5-(4-Phenoxybutoxy)psoralen
Target:
Research Areas:
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
9
9 Cited Publications
Research Areas:
W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 μM, respectively. W-7 hydrochloride induces apoptosis and has antitumor and vascular relaxing activity. W-7 hydrochloride is a blocker of Kv4.3 and can be used for research of arrhythmias .
9
9 Cited Publications
Cat. No.: HY-130368
CAS No.: 65595-90-6
Research Areas:
W-7 is a selective calmodulin antagonist. W-7 inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 μM, respectively. W-7 induces apoptosis and has antitumor and vascular relaxing activity. W-7 is a blocker of Kv4.3 and can be used for research of arrhythmias .
6
Target:
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NNC 55-0396 (NNC 55-0396 dihydrochloride) is a blood-brain-barrier-permeable T-type Ca 2+ channel inhibitor and pan-P450 inhibitor. NNC 55-0396 selectively inhibits T-type Ca 2+ channels, suppresses HIF-1α expression and stability and inhibits Kv currents. NNC 55-0396 reduces brain infarct and attenuates neurological dysfunction. NNC 55-0396 inhibits the activity of multiple P450 enzymes. NNC 55-0396 (free base) can be used for the research of brain injury, hypertension, and glioblastoma .
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Research Areas:
Mosapride is an orally active gastroenterokinetic compound. Mosapride is a 5HT4 agonist. Mosapride is a CYP inducer. Mosapride has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride can be used in the study of gastrointestinal diseases .
6
6 Cited Publications
Cat. No.: HY-B0189A
CAS No.: 112885-42-4
Synonyms: TAK-370 citrate; AS-4370 citrate
Research Areas:
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
6
6 Cited Publications
Cat. No.: HY-B0189B
CAS No.: 636582-62-2
Synonyms: TAK-370 citrate dihydrate; AS-4370 citrate dihydrate
Research Areas:
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM . Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo .
6
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MDL12330A (RMI12330A) is an adenylyl cyclases inhibitor. MDL12330A can inhibit KV channels, increases insulin secretion and Ca 2+ levels. MDL12330A accentuates contractions in uterine rings and inhibits cardiac functions. MDL12330A can be used for the research of endocrinology, metabolic and cardiovascular disease .
3
3 Cited Publications
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Research Areas:
XE991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively .
3
3 Cited Publications
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XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively .
3
3 Cited Publications
Synonyms: RSD1235 hydrochloride
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Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
3
3 Cited Publications
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ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells .
2
2 Cited Publications
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RY796 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with IC50s of 0.25 μM and 0.09 μM for KV2.1 and KV2.2. RY796 has analgesic activity .
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Research Areas:
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue .
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Azetukalner (XEN1101) is a selective and orally active Kv7.2/Kv7.3 potassium channel opener with an EC50 of 27 nM. Azetukalner is approximately 4-fold more selective for Kv7.2/7.3 over Kv7.3/7.5 (EC50 of 94 nM) and Kv7.4 (EC50 of 113 nM) channels. Azetukalner exhibits a selectivity >100-fold for Kv7 channels over other ion channels and receptors. Azetukalner can be used for the study of focal epilepsy .
1
1 Cited Publications
Research Areas:
DPO-1 is a potent Kv1.5 and Kv1.3 (EC50 = 3.1 μM) channels inhibitor with potential immunomodulatory and anti-inflammatory effects. DPO-1 reduces Kv1.3 current density, blunts Ca 2+ influx in Ca 2+-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. DPO-1 inhibits Uric acid sodium (HY-B2130A) (MSU)-induced NLRP3 inflammasome activation by blocking Kv1.5-mediated K + efflux. DPO-1 can be used for the study of immunologic disorders and atrial fibrillation .
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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
