Search Result
Results for "
cerebellar
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B1442
-
N-Acetyl-DL-leucine
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Drug Derivative
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Neurological Disease
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Acetylleucine (N-Acetyl-DL-leucine), orally active compound, can be used for the research of acute vestibular vertigo, cerebellar ataxia and nystagmus .
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- HY-W259932
-
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Ligands for E3 Ligase
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Cancer
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Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker .
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- HY-50707
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(Rac)-T-Type calcium channel inhibitor
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Calcium Channel
Drug Isomer
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Neurological Disease
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(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
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- HY-10035A
-
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Calcium Channel
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Neurological Disease
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(R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
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- HY-19434
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Trans-(±)-ACP
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mGluR
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Metabolic Disease
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trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
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- HY-163169
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Ligands for E3 Ligase
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Others
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Phenyl-glutarimide 4 ’-oxyacetic acid is a carboxylic acid-functionalized cerebellar ligand that can be used in the development of PROTAC deactivators. Phenyl-glutarimide 4 ’-oxyacetic acid binds to PROTAC has better hydrolytic stability and efficacy .
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- HY-117903A
-
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Smo
Hedgehog
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Cancer
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MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
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- HY-157566
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Ligands for E3 Ligase
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Cancer
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Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated .
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- HY-P2628
-
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Fluorescent Dye
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Others
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Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
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- HY-103556
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mGluR
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Neurological Disease
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YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity and neuroprotective properties in vivo. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki value of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 value of 8.6 nM. YM-202074 fumarate can be used in stroke research .
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- HY-W677042
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5α-Androst-16-en-3α-ol
|
GABA Receptor
|
Neurological Disease
|
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and human male axillary sweat. α-Androstenol is also a positive modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50=0.4 μM). α-Androstenol decreases immobility time in the forced swim test and increases time spent in the open arms of the elevated plus maze in mice. α-Androstenol protects against seizures induced by Pentylenetetrazole or electroshock with anxiolytic-like activity in mice .
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- HY-P1987
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Calcium Channel
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Neurological Disease
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Mast cell degranulating peptide (28-49) is a depolarizing agent from bee venom, it can raise the content of cGMP level in mouse cerebellar slices .
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- HY-139097
-
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Acyltransferase
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Others
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C12-Sphingosine is a short-chain Sphingosine homologue. C12-Sphingosine inhibits serine palmitoyltransferase activity in primary cultured cerebellar cells .
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- HY-101316
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NO Synthase
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Neurological Disease
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TRIM is a potent nitric oxide synthase inhibitor. TRIM inhibits mouse cerebellar nNOS and rat lung iNOS in vitro with IC50 values of 28.2 and 27.0 µM, respectively. Antidepressant- and anxiolytic-like effects .
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- HY-161132
-
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E3 Ligase Ligand-Linker Conjugates
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Others
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Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .
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- HY-B1740
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Microtubule/Tubulin
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Neurological Disease
|
Pregnenolone acetate (compound #43), a nonmetabolized Pregnenolone (HY-B0151) analog, can promote neurite extension and induce a change in growth cone morphology in primary cultures of cerebellar granule neurons. Pregnenolone acetate, a neurosteroid, increases microtubule polymerization. Pregnenolone acetate has the potential for neurodevelopmental diseases research .
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- HY-133956
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NSC 680434
|
Apoptosis
CDK
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Neurological Disease
Cancer
|
3-ATA (NSC 680434) is a selective inhibitor of cyclin-dependent kinase 4 (CDK4) with neuroprotective and antitumor effects. 3-ATA can alleviate kainic acid (HY-N2309)-induced apoptosis in cerebellar granule neurons, which can be used in the study of neurodegenerative diseases .
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-
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- HY-117764
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mGluR
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Neurological Disease
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LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
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- HY-137494
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GABA Receptor
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Neurological Disease
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Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam .
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- HY-P3779
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Aβ(17-42)
|
Apoptosis
|
Neurological Disease
|
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
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- HY-B1716
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L-5-HTP; Oxitriptan
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
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L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia .
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-
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- HY-102070
-
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Potassium Channel
|
Neurological Disease
|
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias .
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- HY-100813
-
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GABA Receptor
|
Neurological Disease
Inflammation/Immunology
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Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats .
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-
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- HY-Y0537E
-
|
Biochemical Assay Reagents
Potassium Channel
Calcium Channel
|
Neurological Disease
|
Potassium chloride, for cell culture is potassium chloride that can be used for cell culture. Potassium chloride, for cell culture increases extracellular potassium ion concentration to induce cellular depolarization, thereby activating voltage-gated calcium channels and regulating intracellular calcium signaling. Potassium chloride, for cell culture upregulates Brn-5. Potassium chloride, for cell culture inhibits the proliferation of neurons and some plant cells .
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-
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- HY-130553
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β-NAAG; β-N-Acetylaspartylglutamic acid
|
Aminopeptidase
mGluR
|
Neurological Disease
|
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies .
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-
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- HY-16219
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Gd-EOB-DTPA disodium; ZK 139834
|
Biochemical Assay Reagents
|
Cancer
|
Gadoxetate (Gd-EOB-DTPA) Disodium is a contrast agent in magnetic resonance imaging (MRI) of the hepatobiliary system, which accumulates in normal, functioning hepatocytes. Gadoxetate Disodium aggravates liver fibrosis (LF) induced gadolinium deposition in the liver and deep cerebellar nuclei (DCN) of rats without significant acute histological alterations. Gadoxetate Disodium is used to evaluate focal liver lesions, such as hepatocellular carcinoma or dysplastic nodules .
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-
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- HY-100781
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D-APB; D-2-Amino-4-phosphonobutyric acid
|
iGluR
|
Neurological Disease
|
D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co 2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM) .
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- HY-107717
-
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iGluR
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Neurological Disease
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MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .
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- HY-107510
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mGluR
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Neurological Disease
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YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
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- HY-103312
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(-)-Xestospongin C
|
Calcium Channel
Apoptosis
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Neurological Disease
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Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells .
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- HY-B1716R
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L-5-HTP (Standard); Oxitriptan (Standard)
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Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
L-5-Hydroxytryptophan (Standard) is the analytical standard of L-5-Hydroxytryptophan. This product is intended for research and analytical applications. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia .
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- HY-B1716S
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L-5-HTP-d3; Oxitriptan-d3
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[1]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[2][3][4][5].
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-
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- HY-B1716S1
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L-5-HTP-d3-1; Oxitriptan-d3-1
|
Endogenous Metabolite
|
Metabolic Disease
|
L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan[1]. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[2]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[3][4][5][6].
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- HY-15116
-
|
Prolyl Endopeptidase (PREP)
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Neurological Disease
|
ONO 1603, a novel prolyl endopeptidase inhibitor investigated as a potential antidementia drug, demonstrated neuroprotective and neurotrophic effects in cerebellar granule cells similar to tetrahydroaminoacridine (THA). At a concentration of 0.03 microM, ONO 1603 promoted neuronal survival, enhanced neurite outgrowth, increased m3-muscarinic acetylcholine receptor (mAChR) mRNA levels, and stimulated mAChR-mediated signaling pathways. These findings suggest that ONO 1603 shares pharmacological similarities with THA, indicating its potential as a therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and neuronal function .
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- HY-B1716S2
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L-5-HTP-d4; Oxitriptan-d4
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Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
L-5-Hydroxytryptophan-d4 (L-5-HTP-d4; Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia .
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-
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- HY-157959
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(±)-Orphenadrine
|
iGluR
Cytochrome P450
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
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-
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- HY-10035
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TTA-P2
3 Publications Verification
T-Type calcium channel inhibitor
|
Calcium Channel
|
Neurological Disease
|
TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .
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HY-L086
-
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2,967 compounds
|
Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.
MCE offers a unique collection of 2,967 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.
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Cat. No. |
Product Name |
Type |
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- HY-P2628
-
|
Fluorescent Dyes/Probes
|
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
|
Cat. No. |
Product Name |
Type |
-
- HY-Y0537E
-
|
Buffer Reagents
|
Potassium chloride, for cell culture is potassium chloride that can be used for cell culture. Potassium chloride, for cell culture increases extracellular potassium ion concentration to induce cellular depolarization, thereby activating voltage-gated calcium channels and regulating intracellular calcium signaling. Potassium chloride, for cell culture upregulates Brn-5. Potassium chloride, for cell culture inhibits the proliferation of neurons and some plant cells .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2628
-
|
Fluorescent Dye
|
Others
|
Dabcyl-YVADAPV-EDANS is a fluorogenic interleukin-1β converting enzyme (ICE) substrate for measuring ICE-like protease activity. Dabcyl-YVADAPV-EDANS detects fluorescence at 360 nm excitation and 480 nm emission wavelengths. ICE-like protease is a critical mediator of K + deprivation-induced apoptosis of cerebellar granule neurons .
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-
- HY-P1987
-
|
Calcium Channel
|
Neurological Disease
|
Mast cell degranulating peptide (28-49) is a depolarizing agent from bee venom, it can raise the content of cGMP level in mouse cerebellar slices .
|
-
- HY-P3779
-
Aβ(17-42)
|
Apoptosis
|
Neurological Disease
|
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
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- HY-B1716S
-
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L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[1]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[2][3][4][5].
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- HY-B1716S2
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L-5-Hydroxytryptophan-d4 (L-5-HTP-d4; Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia .
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- HY-B1716S1
-
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L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan[1]. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[2]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[3][4][5][6].
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Cat. No. |
Product Name |
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Classification |
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- HY-161132
-
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Azide
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Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .
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