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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
26 Results for "
GIRK
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "GIRK" 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 .
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Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis .
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11 Cited Publications
Synonyms: NP-120 tartrate; RC-61-91 tartrate
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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 .
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11 Cited Publications
Synonyms: BAF-312 hemifumarate
Target:
Research Areas:
Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis .
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3 Cited Publications
Cat. No.: HY-P1275
CAS No.: 910044-56-3
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2 Cited Publications
Synonyms: VU 0456810; CID 56642816
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ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 can cross the blood-brain barrier with brain-to-plasma ratio of 0.2 in mice model (i.p.). ML 297 is potential for the treatment of epilepsy .
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1 Cited Publications
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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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1 Cited Publications
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Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron . Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect .
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VU0529331 is a homomeric GIRK channel activator, with an EC50 value of 5.1 μM for human GIRK2 and an EC50 value of 22.3 μM for GIRK4. VU0529331 serves as a starting point for the development of non-GIRK1/X channel probes and also acts as a tool for studying homomeric GIRK channels. VU0529331 is applicable to research related to addiction, primary aldosteronism and delayed-onset obesity .
Research Areas:
RTI-7470-44 is an orally active and blood-brain barrier-permeable antagonist of trace amine-associated receptor 1 (hTAAR1) with a Ki of 0.3 nM. RTI-7470-44 inhibits hTAAR1-mediated cAMP production and signal transduction (IC50 = 8.4 nM), and blocks hTAAR1-mediated GIRK current responses. RTI-7470-44 increases the spontaneous firing frequency of dopaminergic neurons and reduces collagen-induced platelet aggregation. RTI-7470-44 can be used in studies related to Parkinson's disease and gastric emptying .
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RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2) . RU-TRAAK-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-12355S
CAS No.: 2104759-32-0
Synonyms: BAF-312-d11
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Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine subsequently activates VTA dopamine neuron . Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect .
Cat. No.: HY-108400
CAS No.: 87134-87-0
Synonyms: R-(+)-SCH-23390 maleate
Research Areas:
SCH-23390 maleate (R-(+)-SCH-23390 maleate) 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 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
Cat. No.: HY-122647
CAS No.: 1976050-09-5
Synonyms: VU0652957; VU2957
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Research Areas:
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .
Cat. No.: HY-12355R
CAS No.: 1230487-00-9
Synonyms: BAF-312 (Standard)
Research Areas:
Siponimod (BAF-312) (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.
Cat. No.: HY-12520B
CAS No.: 81702-42-3
Synonyms: (±)-SKF-38393 hydrochloride; SKF-38393A hydrochloride
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(R)-SKF 38393 ((±)-SKF-38393) hydrochloride is a potent and selective D1 dopamine receptor antagonist. (R)-SKF 38393 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channel .
Cat. No.: HY-12882AR
CAS No.: 23210-58-4
Synonyms: NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)
Cat. No.: HY-117403
CAS No.: 1801338-22-6
AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC50 values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms .
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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
