Search Result
Results for "
rat brain
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P1519B
-
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BNP (1-32), rat acetate
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Angiotensin Receptor
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Cardiovascular Disease
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Brain Natriuretic Peptide (1-32), rat acetate (BNP (1-32), rat acetate) is a 32 amino acid polypeptide secreted by the ventricles of the heart in response to excessive stretching of heart muscle cells (cardiomyocytes) .
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- HY-150209
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Others
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Neurological Disease
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MODAG-001 can bind to synuclein fibrils in a rat brain. MODAG-001 is a candidate α-syn imaging probe .
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- HY-P3219
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Endogenous Metabolite
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Endocrinology
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N-Acetyloxytocin is isolated and characterized in the neurointermediate lobe of the rat pituitary (NIL) and their presence in several brain areas of the rat .
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- HY-N0435
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Others
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Neurological Disease
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Isorhamnetin 3-gentiobioside protects the morphological structures and restores acetylcholine level in rat hippocampus, and improves brain functions via normalizing brain EEG .
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-
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- HY-109012A
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JNJ-42847922 hydrochloride
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Orexin Receptor (OX Receptor)
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Neurological Disease
Endocrinology
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Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
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- HY-P1519
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BNP (1-32), rat
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Angiotensin Receptor
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Cardiovascular Disease
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Brain Natriuretic Peptide (1-32), rat (BNP (1-32), rat) is a 32 amino acid polypeptide secreted by the ventricles of the heart in response to excessive stretching of heart muscle cells (cardiomyocytes) .
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- HY-P2457
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Bacterial
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Infection
Inflammation/Immunology
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rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS .
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- HY-120965
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Endogenous Metabolite
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Metabolic Disease
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Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered. N-Palmitoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling. Its function is currently under investigation.
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- HY-N13258
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β-Citrylglutamic acid
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Others
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Others
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β-Citryl-L-glutamic acid (β-Citrylglutamic acid) is a citrylglutamic acid, that can be isolated from newborn rat brain .
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- HY-120325
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Others
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Cardiovascular Disease
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DHMPA is an effective depletor of norepinephrine content of the heart, brain and spleen in mouse and rat. DHMPA has antihypertensive effects .
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- HY-109012
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JNJ-42847922
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Orexin Receptor (OX Receptor)
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Neurological Disease
Endocrinology
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Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
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- HY-P1090
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
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- HY-120963
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Endogenous Metabolite
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Metabolic Disease
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Several different arachidonoyl amino acids, including N-arachidonoyl dopamine and N-arachidonoyl serine, have been isolated and characterized from bovine brain.1 During mass spectral lipidomics analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, were discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Oleoyl taurine is an amino-acyl endocannabinoid isolated from rat brain that may activate TRPV1 and TRPV4.
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- HY-120964
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Endogenous Metabolite
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Metabolic Disease
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Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Stearoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling.
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- HY-15084
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(+)-MK 801 Maleate
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iGluR
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Neurological Disease
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Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
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- HY-119061
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5-HT Receptor
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Neurological Disease
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SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .
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- HY-P1090A
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
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- HY-19740
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- HY-13929
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Monoamine Oxidase
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Neurological Disease
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Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro .
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- HY-P1303
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-P1303A
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-130238
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(±)8-HDoHE; 8-hydroxy Docosahexaenoic acid; (±)8-HDoHE
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Endogenous Metabolite
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Metabolic Disease
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(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
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- HY-130287
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(±)16-HDoHE; 16-hydroxy Docosahexaenoic acid; (±)16-HDoHE
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Endogenous Metabolite
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Metabolic Disease
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(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)16-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
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- HY-100792
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Bacterial
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Cancer
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URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
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- HY-P3964
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Endogenous Metabolite
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Endocrinology
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TRH Precursor Peptide is a precursor peptide of thyrotropin-releasing hormone (TRH). TRH Precursor Peptide formation of TRH in rat brain and pituitary is zinc-dependent .
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- HY-100821
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Bacterial
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Infection
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2,4-Dihydroxyphenylacetylasparagine is a potent and selective antagonist of glutamate. 2,4-Dihydroxyphenylacetylasparagine inhibits glutamate binding to rat brain synaptic membranes .
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- HY-114651
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Others
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Cancer
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Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitory activity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice .
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- HY-108295
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CXB-722
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GABA Receptor
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Neurological Disease
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Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
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- HY-P1134
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5-HT Receptor
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Neurological Disease
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Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
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- HY-N2070
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Na+/K+ ATPase
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Neurological Disease
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Acevaltrate inhibits the Na +/K +-ATPase activity in the rat kidney and brain hemispheres with IC50s of 22.8 μM and 42.3 μM, respectively .
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- HY-113516
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- HY-108616
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Phospholipase
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Cancer
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VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research .
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- HY-129665
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(±)-O,O-Dimethylcoclaurine
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Endogenous Metabolite
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Metabolic Disease
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GS 389 ((±)-O,O-Dimethylcoclaurine) is a tetrahydroisoquinoline. GS-389 inhibites Cyclic AMP and cyclic AMP dependent phosphodiesterases from rat atrial and ventricular tissue. GS-389 relaxes the contraction induced by phenylephrine and high K + in rat aortic rings .
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- HY-120710
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- HY-119095
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- HY-123594
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Cannabinoid Receptor
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Neurological Disease
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R-2 Methanandamide (Compound 2) is a cannabinoid Anandamide (HY-10863) analog with a Ki of 119 nM for the cannabinoid receptor (Ki is determined using rat brain membranes with PMSF) .
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- HY-10936
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iGluR
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Neurological Disease
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S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests .
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- HY-135507
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5-HT Receptor
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Neurological Disease
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NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions .
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- HY-128976
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DHED
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Estrogen Receptor/ERR
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Metabolic Disease
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10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor proagent of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain .
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- HY-12332
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JW 642
2 Publications Verification
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MAGL
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Neurological Disease
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JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
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- HY-108973
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5-HT Receptor
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Neurological Disease
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CGP 15210G is an inhibitor of 5-HT reuptake. CGP 15210G inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo .
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- HY-B1237A
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil hydrochloride hydrochloride is an active agent against on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes. Suloctidil hydrochloride is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders.
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- HY-10864
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URB-597
5 Publications Verification
KDS-4103
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FAAH
Autophagy
Mitophagy
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Neurological Disease
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URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
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- HY-12567
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VU0483253
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mAChR
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Neurological Disease
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ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .
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- HY-121810
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Others
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Others
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LBT-999 is a phenyltropane derivative used for positron emission tomography (PET) exploration of the dopamine transporter (DAT). It has high affinity binding to DAT on rat striatal membranes and human postmortem brain slices in vitro, high uptake in the striatum in rat and baboon models in vivo, and its binding can be blocked by specific compounds.
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- HY-104003
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- HY-104003A
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Histamine Receptor
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Neurological Disease
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S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
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- HY-B1237
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil is a new drug that is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders
Target：
Effect of suloctidil on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes.
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- HY-139802
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Others
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Others
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L-779976 is a compound with bradykinin agonist activity. Injection into the amygdala and septum of the rat brain can produce anxiolytic effects. Its bradykinin agonist activity has been verified by relevant experiments.
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- HY-103169
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Adenosine Receptor
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Neurological Disease
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SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain .
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- HY-15112
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Prolyl Endopeptidase (PREP)
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Infection
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JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096) .
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- HY-18610
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Ro 8-4650 hydrochloride
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Dopamine Transporter
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Neurological Disease
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Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
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- HY-18610A
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Ro 8-4650
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Dopamine Transporter
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Neurological Disease
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Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
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- HY-19301
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J-104135
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Farnesyl Transferase
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Cancer
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J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP) .
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- HY-119127
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Cholecystokinin Receptor
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Metabolic Disease
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TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCKA receptors (IC50=1.2 nM) than to rat brain CCKB receptors (IC50=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases .
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- HY-116663
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(±)20-HDoHE
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Endogenous Metabolite
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Neurological Disease
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(±)20-HDHA ((±)20-HDoHE) is a racemic mixture and is an autoxidation product of Docosahexaenoic acid (DHA). (±)20-HDHA is also formed by peroxidation process in human platelets and rat brain homogenate .
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- HY-100998
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iGluR
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Neurological Disease
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Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates . Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms .
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- HY-120369
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FAAH
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Neurological Disease
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URB532 is an inhibitor for fatty acid amide hydrolase (FAAH) with an IC50 of 396 nM. URB532 increases levels of arachidonic acid acetamide (AEA), palmitoylethanolamide (PEA), and oleamide (OEA) in the rat brain, and exhibits anxiolytic and analgesic effects .
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- HY-13929R
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Monoamine Oxidase
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Neurological Disease
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Isocarboxazid (Standard) is the analytical standard of Isocarboxazid. This product is intended for research and analytical applications. Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro .
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- HY-106224B
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Hypocretin-1 (human, rat, mouse) (acetate)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .
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- HY-12959A
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BAY x 3702
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5-HT Receptor
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Neurological Disease
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Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
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- HY-14200A
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TVP1022 mesylate; S-PAI mesylate
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Monoamine Oxidase
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Neurological Disease
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(S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
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- HY-N2080
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GABA Receptor
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Cancer
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Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .
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- HY-100605
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mGluR
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Others
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VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively .
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- HY-101169
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Monoamine Oxidase
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Neurological Disease
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Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
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- HY-107686
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5-I A-85380 dihydrochloride
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nAChR
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Neurological Disease
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5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
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- HY-10712
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GlyT
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Neurological Disease
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Org-24598 is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 can inhibit the specific binding of [ 3H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM .
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- HY-107562
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Histamine Receptor
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Neurological Disease
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JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research .
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- HY-121191
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N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
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Cholinesterase (ChE)
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Neurological Disease
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Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
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- HY-12959
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BAY x 3702 free base
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5-HT Receptor
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Neurological Disease
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Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects .
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- HY-121156
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LF 16-0687; XY-2405
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Bradykinin Receptor
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Neurological Disease
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Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
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- HY-130288
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(±)13-HDoHE; 13-hydroxy Docosahexaenoic acid; (±)13-HDoHE
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Others
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Inflammation/Immunology
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(±)13-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. Fresh water hydra is shown to metabolize DHA to 13(R)-HDHA, presumably via the 11R-lipoxygenase activity. (±)13-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
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-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
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-
- HY-100937
-
|
PD 116948
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes .
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-
- HY-126644
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Halocyamine B exhibits antimicrobial activity against a variety of bacteria and yeasts. Halocyamine B exhibits cytotoxicity to cultured neural cells of rat fetal brain, mouse neuroblastoma N18 cells, and human hepatoma HepG2 cells .
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-
- HY-120463
-
|
|
PKC
|
Cancer
|
|
R8605 is an inhibitor for PKC with an IC50 of 65 μM for PKC in rat brain. R8605 inhibits calcium/phospholipid-independent phosphorylation of protamine with IC50 of 70 μM and 100 μM. R8605 can be used in cancer research .
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-
- HY-168167
-
|
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Others
|
Neurological Disease
|
|
BuChE-IN-14 is a novel compound that selectively inhibits acetylcholinesterase (AChE) activity. BuChE-IN-14 showed a concentration-dependent inhibitory effect on AChE in rat brain in vitro experiments. BuChE-IN-14 can increase the extracellular acetylcholine (ACh) concentration in the rat hippocampus and striatum at a certain dose. BuChE-IN-14 may help improve memory impairment caused by cholinergic dysfunction .
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-
- HY-10713
-
|
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GlyT
|
Neurological Disease
|
|
Org-24598 lithium is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 lithium can inhibit the specific binding of [ 3H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM .
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-
- HY-14174
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduce Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) .
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-
- HY-16923A
-
|
BIII-890 hydrochloride; BIII-890 CL
|
Sodium Channel
|
Neurological Disease
|
|
Crobenetine hydrochloride (BIII-890 hydrochloride) is the hydrochloride form of Crobenetine (HY-16923). Crobenetine hydrochloride is a selective inhibitor for Na + channel. Crobenetine hydrochloride displaces 3HBTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, exhibits only low binding affinity for other receptors and ion channels. Crobenetine hydrochloride protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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-
- HY-110180
-
|
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
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-
- HY-19225
-
|
KA-672 hydrochloride; Anseculin hydrochloride
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Others
|
Neurological Disease
|
Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems .
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-
- HY-59201A
-
|
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
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-
- HY-107688A
-
|
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- HY-107688
-
|
|
nAChR
|
Neurological Disease
|
|
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- HY-101478A
-
|
|
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
|
-
- HY-119282
-
|
|
mGluR
|
Neurological Disease
|
|
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
|
-
- HY-19310
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
AMP-579 is an adenosine receptor agonist that primarily targets adenosine A1 and A2A receptors (with Ki values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a Ki value of 56 nM for the A2A receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of A2A receptors (with an IC50 of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction .
|
-
- HY-16923
-
|
BIII-890; BIII-890 CL free acid
|
Sodium Channel
|
Neurological Disease
|
|
Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
|
-
- HY-14450
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-31020028 is a selective and brain penetrant antagonist of neuropeptide Y Y2 receptor with pIC50 values of 8.07 and 8.22 for human and rat Y2 receptor, respectively. JNJ-31020028 can be used for the research of nervous disease .
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-
- HY-N2160
-
|
|
GABA Receptor
|
Neurological Disease
|
|
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons .
|
-
- HY-15084B
-
Dizocilpine
Maximum Cited Publications
27 Publications Verification
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
|
-
- HY-44157
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain .
|
-
- HY-NP019
-
|
|
Sirtuin
Caspase
Apoptosis
|
Neurological Disease
|
|
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
|
-
- HY-162663
-
|
ML253
|
mAChR
|
Neurological Disease
|
|
VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic .
|
-
- HY-B1614
-
-
- HY-136233
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-136233A
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium hydrate has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research .
|
-
- HY-N7062
-
|
Takeda-25
|
FAAH
|
Neurological Disease
|
|
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics .
|
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-130748
-
|
|
Others
|
Infection
|
|
K-252d is an indolocarbazole alkaloid found in Nocardiopsis. It is a PKC inhibitor that inhibits PKC isolated from rat brain (IC50=350 nM). It also inhibits calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart (IC50=46.2 μM).
|
-
- HY-110016
-
|
DEA
|
Endogenous Metabolite
Cannabinoid Receptor
|
Neurological Disease
|
|
Docosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a Ki value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system .
|
-
- HY-W020468
-
|
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-N2326
-
|
|
nAChR
|
Neurological Disease
|
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
|
-
- HY-P3071
-
|
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
|
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
|
-
- HY-119226
-
|
|
mAChR
|
Neurological Disease
|
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
|
-
- HY-18698
-
|
|
iGluR
|
Neurological Disease
|
|
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
|
-
- HY-U00322
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM .
|
-
- HY-100125
-
|
SR1368
|
COX
|
Inflammation/Immunology
|
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- HY-N0745
-
|
|
Caspase
|
Inflammation/Immunology
|
|
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3 .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-120170
-
|
|
ASCT
Adrenergic Receptor
Dopamine Transporter
|
Neurological Disease
|
|
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [ 3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research .
|
-
- HY-118256
-
|
|
mGluR
|
Neurological Disease
|
|
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research .
|
-
- HY-113149
-
|
|
Endogenous Metabolite
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Argininosuccinic acid participates in the fourth step of the urea cycle, with being cleaved to arginine and fumaric acid by argininosuccinic acid lyase (ASL). Argininosuccinic acid reduces reduced glutathione (GSH) level, and increases the production of reactive oxygen species in cerebral cortex and striatum. Argininosuccinic acid causes lipid peroxidation and protein oxidation, and induces oxidative stress in the developing rat brain .
|
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-18138
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .
|
-
- HY-120547
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
UCB-11056 is a modulator of cyclic AMP generation. UCB-11056 can rapidly increase cyclic AMP levels in the rat brain in vivo and potentiate stimulated cyclic AMP formation in vitro. UCB-11056 does not stimulate cAMP formation on its own. UCB-11056 is a potential nootropic drug .
|
-
- HY-161965
-
|
|
FAAH
|
Neurological Disease
|
|
MK-3168 (12C) is a FAAH inhibitor with IC50 values of 1.0, 5.5, 1.7 nM for human, rhesus, rat, respectively. MK-3168 shows good brain uptake and FAAH-specific signal. 11C MK-3168 can be used as FAAH PET tracer .
|
-
- HY-116673
-
|
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
|
-
- HY-116062A
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
|
-
- HY-106301
-
|
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-103304
-
|
|
Others
|
Neurological Disease
|
|
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .
|
-
- HY-113149A
-
|
|
Endogenous Metabolite
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Argininosuccinic acid disodium participates in the fourth step of the urea cycle and is cleaved into arginine and fumarate by argininosuccinate lyase (ASL). Argininosuccinic acid disodium reduces reduced glutathione (GSH) concentrations and increases reactive oxygen species production in the cerebral cortex and striatum. Argininosuccinic acid disodium causes lipid peroxidation and protein oxidation and also induces oxidative stress in the developing rat brain .
|
-
- HY-P4052
-
|
|
ROS Kinase
|
Neurological Disease
|
|
Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygen species (ROS) accumulation and suppresses the activation of ERK 1/2. Pinealon stimulates the functional activity of the main cellular elements of brain tissue, reduces the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia .
|
-
- HY-131693A
-
|
GAG hydrochloride
|
GABA Receptor
|
Neurological Disease
Cancer
|
|
γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA hydrochloride can increase the concentration of GABA in rat brain . γ-Acetylenic GABA (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-156331
-
|
|
mGluR
|
Neurological Disease
|
|
VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-W795507
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
|
-
- HY-116062
-
|
|
Others
|
Others
|
|
JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
|
-
- HY-165116
-
|
18:0p/22:6-PE; C18(Plasm)-22:6-PE; PE(P-18:0/22:6)
|
Others
|
Others
|
|
1-1(Z)-Octadecenyl-2-docosahexaenoyl-sn-glycero-3-PE (18:0p/22:6-PE) is a lipid identified in rat brain tissue by mass spectrometry imaging with specific structural and distribution characteristics, and isomers of different fatty acid chains can be identified by improved methods.
|
-
- HY-B1614R
-
|
|
Adrenergic Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Clenbuterol (hydrochloride) (Standard) is the analytical standard of Clenbuterol (hydrochloride). This product is intended for research and analytical applications. Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
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Others
Neurological Disease
Metabolic Disease
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[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
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![[Glp5,(Me)Phe8,Sar9] Substance P (5-11)](//file.medchemexpress.eu/product_pic/hy-p3801.gif)
- HY-107664
-
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Neurotensin Receptor
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Neurological Disease
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SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-107664A
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Neurotensin Receptor
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Neurological Disease
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SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-14605
-
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(R)-AGN1135 mesylate; TVP1012 mesylate
|
Monoamine Oxidase
Autophagy
Apoptosis
|
Neurological Disease
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Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-14605A
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(R)-AGN1135; TVP1012
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Monoamine Oxidase
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Neurological Disease
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Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-126419
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SARS-CoV
PKC
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Infection
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Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM. Kobophenol A inhibits the activity of partially purified rat brain protein kinase C (PKC) with an IC50 of 52 µM .
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- HY-122964
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Cannabinoid Receptor
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Metabolic Disease
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URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity .
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- HY-158374
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IRAK
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Inflammation/Immunology
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BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
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- HY-13290
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CaMK
P2X Receptor
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Metabolic Disease
Cancer
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KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
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- HY-14200
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TVP1022; S-PAI
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Monoamine Oxidase
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Neurological Disease
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(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-19578B
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(±)-Isamoltane hemifumarate
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity .
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- HY-12439
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ML380
1 Publications Verification
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mAChR
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Neurological Disease
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ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
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- HY-101368A
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Bradykinin Receptor
mAChR
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Neurological Disease
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WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
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- HY-15008
-
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Oxytocin Receptor
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Endocrinology
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L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor .
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- HY-106808
-
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IOS-1.1212
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Calcium Channel
Chloride Channel
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Neurological Disease
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Cerebrocrast (IOS-1.1212) is a 1,4-dihydropyridine (DHP) derivative. Cerebrocrast has a high affinity for the membrane lipid bilayer and it can easily penetrate the blood-brain barrier and incorporate into the plasma and organelle membranes, including those of mitochondria. Cerebrocrast promotes the cotransport of H+ and Cl- in rat liver mitochondria. Cerebrocrast also exhibits neuroprotective and cognition enhancer properties .
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- HY-111066
-
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Others
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Others
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JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
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- HY-10061
-
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AZD-3355
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GABA Receptor
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Metabolic Disease
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Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-102064
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5-HT Receptor
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Neurological Disease
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SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
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- HY-10061B
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AZD-3355 hydrochloride
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GABA Receptor
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Metabolic Disease
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Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-131693
-
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GAG
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GABA Receptor
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Neurological Disease
Cancer
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γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain . γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P3883
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![[DAla4] Substance P (4-11)](//file.medchemexpress.eu/product_pic/hy-p3883.gif)
- HY-118210
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FAAH
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Metabolic Disease
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PHOP is a fatty acid amide hydrolase (FAAH) inhibitor used to assess inhibitory activity in a fluorometric assay. PHOP can determine FAAH activity by measuring the amount of 4-pyridin-1-ylbutyric acid released by the enzyme in rat brain microsomes. PHOP demonstrates potential as a FAAH inhibitor and can directly measure FAAH activity by reversed-phase HPLC and fluorescence detection, providing a basis for the development of new inhibitors.
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- HY-106874B
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rel-RS-15385-197
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Adrenergic Receptor
Prostaglandin Receptor
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Neurological Disease
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rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
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- HY-101478
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mGluR
Apoptosis
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Neurological Disease
Cancer
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Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
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- HY-110160
-
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ABT-089 dihydrochloride
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nAChR
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Neurological Disease
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Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
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- HY-129624A
-
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Ro 31-7549 acetate; Bis VIII acetate
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PKC
Apoptosis
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Inflammation/Immunology
Cancer
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Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively . Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases .
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- HY-P1318
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Opioid Receptor
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Neurological Disease
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Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
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- HY-P1318A
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Opioid Receptor
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Neurological Disease
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Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
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- HY-10061A
-
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AZD-3355 napadisylate
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GABA Receptor
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Metabolic Disease
|
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Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
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- HY-109509
-
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PK 10169; Enoxaparin sodium
|
Factor Xa
Thrombin
SARS-CoV
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
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Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19 .
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- HY-14605S
-
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(R)-AGN1135-13C3 mesylate; TVP1012-13C3 mesylate
|
Isotope-Labeled Compounds
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Others
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Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylateis the deuterium labeledRasagiline (mesylate)(HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively .
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- HY-106301R
-
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Cholecystokinin Receptor
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Metabolic Disease
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Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
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- HY-B0573
-
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Adrenergic Receptor
Bacterial
|
Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
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Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
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- HY-B0573B
-
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Adrenergic Receptor
Bacterial
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Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
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Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
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- HY-129624
-
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Ro 31-7549; Bis VIII
|
PKC
Apoptosis
|
Inflammation/Immunology
Cancer
|
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Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively . Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases .
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- HY-129245
-
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Hoe 175
|
Endogenous Metabolite
|
Neurological Disease
|
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Razobazam (Hoe 175) is a benzodiazepine derivative with cognitive activity. Razobazam has been shown to improve learning performance in socially deprived rats. Razobazam increased avoidance scores by 18% after training. Razobazam caused significant changes in the optical density of certain areas of the rat brain, including a 22% decrease in the lateral habenula and a 25% increase in the ventral tegmental area. Razobazam also caused a 13% increase in optical density in the prefrontal cortex of rats .
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- HY-160959
-
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nAChR
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Neurological Disease
|
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AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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- HY-N3807
-
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Acyltransferase
ERK
NF-κB
|
Infection
Cardiovascular Disease
Cancer
|
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Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes . Enniatin B1 crosss the blood-brain barrier . Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation .
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- HY-107732
-
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Neuropeptide Y Receptor
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Neurological Disease
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JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
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- HY-107479
-
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Neuropeptide Y Receptor
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Neurological Disease
|
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(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
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- HY-120124
-
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SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
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Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
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- HY-P5754B
-
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Apoptosis
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Neurological Disease
|
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TAT-NEP1-40 acetate is a therapeutic candidate for axonal regeneration and functional recovery after stroke. TAT-NEP1-40 acetate can protect PC12 cells against oxygen and glucose deprivation (OGD) and promote neurite outgrowth. TAT-NEP1-40 acetate protects the brain against ischemia/reperfusion injury through inhibition of neuronal apoptosis. TAT-NEP1-40 acetate can be efficiently delivered into the rat brains .
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- HY-111283
-
|
(+)-AJ 76; (1S,2R)-AJ 76
|
Dopamine Receptor
|
Neurological Disease
|
|
AJ-76 ((+)-AJ 76; (1S,2R)-AJ 76) is a dopamine autoreceptor antagonist. AJ-76 can increase the synthesis and turnover of dopamine in the rat brain, while having little effect on the synthesis and turnover of serotonin (5-HT) and norepinephrine. AJ-76 can also antagonize the sedative effects of low-dose apomorphine and has a weak antagonistic effect on postsynaptic dopamine receptor .
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- HY-14605AR
-
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Monoamine Oxidase
|
Neurological Disease
|
|
Rasagiline (Standard) is the analytical standard of Rasagiline. This product is intended for research and analytical applications. Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-14605R
-
|
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Monoamine Oxidase
Autophagy
Apoptosis
|
Neurological Disease
|
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Rasagiline (mesylate) (Standard) is the analytical standard of Rasagiline (mesylate). This product is intended for research and analytical applications. Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-160939
-
|
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MAP3K
|
Neurological Disease
Inflammation/Immunology
|
|
ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
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- HY-117931
-
|
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Potassium Channel
|
Neurological Disease
|
|
NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity .
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- HY-103164A
-
|
CSC
|
Others
|
Neurological Disease
|
|
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitory activity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .
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- HY-120596
-
|
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PPAR
|
Neurological Disease
|
|
PPARδ/γ agonist 1 sodium is a chemically unique and brain penetrant dual PPAR delta/gamma agonist. PPARδ/γ agonist 1 sodium can be used for the research of Alzheimer’s disease .
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-
- HY-111191
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment .
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-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-124379
-
TPCK
1 Publications Verification
L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK
|
Ser/Thr Protease
HPV
Apoptosis
PDK-1
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
|
-
- HY-15113A
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) .
|
-
- HY-137672A
-
|
2',3'-cNADP+; β-Nicotinamide adenine dinucleotide-2',3'-cyclic phosphate
|
Others
|
Neurological Disease
|
|
2',3'-Cyclic NADP disodium (2',3'-cNADP+; β-Nicotinamide adenine dinucleotide-2',3'-cyclic phosphate) is a substrate for 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP), an enzyme abundant in myelin. It has been used in a coupled enzyme assay to quantify CNP activity. 2',3'-Cyclic NADP disodium (5 μM) increases calcium overload-induced calcium release and prevents calcium-induced swelling in rat brain mitochondria.
|
-
- HY-15113
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) .
|
-
- HY-100481
-
|
RPR101048
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
|
-
- HY-18137
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
|
-
- HY-13866
-
|
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate
|
PKC
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-13866A
-
|
Bisindolylmaleimide IX
|
PKC
|
Cardiovascular Disease
Neurological Disease
|
|
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-14850
-
|
Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
|
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM . Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively .
|
-
- HY-B0573BS
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-B0573S
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-122608
-
|
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
|
-
- HY-B0573R
-
|
|
Adrenergic Receptor
Bacterial
|
Neurological Disease
Endocrinology
Cancer
|
|
Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
|
-
- HY-168096
-
|
|
NO Synthase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
|
-
- HY-B0573S1
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
- HY-117160
-
|
4-trans-hydroxycyclohexyl Glyburide; 4-trans-hydroxy Glibenclamide
|
Potassium Channel
|
Neurological Disease
|
|
rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide (HY-15206). It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.
|
-
- HY-116450
-
|
|
Others
|
Neurological Disease
|
|
TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
|
-
- HY-14280
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-14280A
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-A0168S
-
|
CVT-3146-d3
|
Adenosine Receptor
|
Cardiovascular Disease
Cancer
|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
|
-
- HY-144790
-
|
|
Amyloid-β
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease .
|
-
- HY-15074
-
|
NS-1209
|
iGluR
|
Neurological Disease
|
|
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
|
-
- HY-15076
-
|
NS-1209 sodium
|
iGluR
|
Neurological Disease
|
|
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
|
-
- HY-130349
-
|
L-656,748
|
Others
|
Infection
|
|
Emamectin B1a is a semisynthetic derivative of avermectin B1a. It binds to GABAA receptors (Ki=17.6 nM in rat brain membranes), including those containing β1, β2, or β3 subunits (IC50s=57, 210, and 49.8 nM for α1β1γ2, α1β2γ2, and α1β3γ2 subunits, respectively), and potentiates the GABA response.2 Emamectin B1a also binds to and inhibits glycine receptors (IC50=218 nM in rat spinal cord). Emamectin B1a induces mortality in 90% of S. exigua larvae in a diet incorporation assay at a dose of 1.067 ng/ml, which is approximately 1,500-fold more toxic than avermectin B1. It is effective against neonate S. eridania larvae in a foliage spray bioassay and when applied topically.
|
-
- HY-14280S
-
|
|
COMT
|
Neurological Disease
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
- HY-14280R
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-B0596
-
|
TA-0910
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-D1056A4
-
|
LPS, from Escherichia coli (O128:B12)
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Lipopolysaccharides, from E. coli O128:B12 is commonly used to stimulate the inflammatory pathway in an infection/inflammation induced preterm animal model. Specific Lipopolysaccharides from E. coli serotypes induce activation of different inflammatory pathways in the neonatal rat brain. Compared with other Escherichia coli, Lipopolysaccharides (O111:B4, O55:B5, O127:B8), Lipopolysaccharides, from E. coli O128:B12 has lower induction efficiency of inflammation. Cub survival rate was 100% after the treatment .
|
-
- HY-N9480
-
|
SM-345431
|
Phospholipase
Bacterial
|
Infection
Cancer
|
|
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A, phospholipase C (PLC) and FabI inhibitor, with IC50s of 0.1-0.2 μM and 0.9 mM for semaphorin3A and FabI. Vinaxanthone inhibits the substrate (t-o-NAC thioester) and the cofactor (NADPH) with Kis of 3.1 μM and 1.0 μM, respectively. Vinaxanthone can be used to handle infections caused by multidrug-resistant pathogens .
|
-
- HY-B0596A
-
|
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-138232
-
|
LTNAM
|
Others
|
Neurological Disease
|
|
Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
|
-
- HY-136625
-
|
|
Others
|
Neurological Disease
|
|
LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT). Its cardiovascular activity was studied in anesthetized spontaneously hypertensive rats (SHR). Acute intraperitoneal injection of 10 and 20 mg/kg of LY134046 caused minimal cardiovascular changes, while 40 mg/kg resulted in a sustained decrease in mean arterial blood pressure and heart rate. This hypotension and bradycardia occurred rapidly and occurred when brain NMT activity was significantly inhibited. However, norepinephrine concentrations in rat brains were not significantly reduced at the time when LY134046-induced blood pressure and heart rate effects were maximal. The acute cardiovascular activity of LY134046 was not significantly affected by pretreatment of SHR with phentolamine, propranolol, or atropine, and LY134046 reduced heart rate in suspended SHR. In addition, acute or chronic administration of LY134046 did not antagonize the vasoconstrictor responses induced by sympathetic nerve stimulation or exogenous norepinephrine. These observations suggest that LY134046 does not interact with adrenergic or cholinergic receptors and that its hypotensive and bradycardic effects do not require neurogenic tension. Chronic intraperitoneal administration of LY134046 (40 mg/kg/day) resulted in a sustained and significant inhibition of hypothalamic and brainstem NMT activity, leading to central norepinephrine depletion. During chronic treatment, norepinephrine and dopamine concentrations increased in the brainstem and hypothalamus of SHR. Despite chronic inhibition of central NMT and norepinephrine depletion, cardiovascular parameters in SHR treated groups were not significantly different from those in saline-injected controls. Chronic treatment with LY134046 did not result in tolerance to its central biochemical effects or acute cardiovascular activity. The present study does not support the idea that norepinephrine-producing neurons are involved in the central regulation of cardiovascular function, because the hypotension and bradycardia induced by acute administration of LY134046 occurred before a significant decrease in hypothalamic norepinephrine concentrations, whereas chronic inhibition of central NMT and depletion of norepinephrine resulted in minimal changes in baseline cardiovascular parameters.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-NP019
-
|
|
Native Proteins
|
|
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
|
-
- HY-D1056A4
-
|
LPS, from Escherichia coli (O128:B12)
|
Carbohydrates
|
|
Lipopolysaccharides, from E. coli O128:B12 is commonly used to stimulate the inflammatory pathway in an infection/inflammation induced preterm animal model. Specific Lipopolysaccharides from E. coli serotypes induce activation of different inflammatory pathways in the neonatal rat brain. Compared with other Escherichia coli, Lipopolysaccharides (O111:B4, O55:B5, O127:B8), Lipopolysaccharides, from E. coli O128:B12 has lower induction efficiency of inflammation. Cub survival rate was 100% after the treatment .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1519B
-
|
BNP (1-32), rat acetate
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Brain Natriuretic Peptide (1-32), rat acetate (BNP (1-32), rat acetate) is a 32 amino acid polypeptide secreted by the ventricles of the heart in response to excessive stretching of heart muscle cells (cardiomyocytes) .
|
-
- HY-P3219
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
N-Acetyloxytocin is isolated and characterized in the neurointermediate lobe of the rat pituitary (NIL) and their presence in several brain areas of the rat .
|
-
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1573
-
|
BNP-45, rat
|
Peptides
|
Cardiovascular Disease
|
|
Brain Natriuretic Peptide-45, rat (BNP-45, rat) is a circulating form of rat brain natriuretic peptide isolated from rat heart with potent hypotensive and natriuretic potency .
|
-
- HY-P1573A
-
|
BNP-45, rat TFA
|
Peptides
|
Cardiovascular Disease
|
|
Brain Natriuretic Peptide-45, rat TFA (BNP-45, rat TFA) is a circulating form of rat brain natriuretic peptide isolated from rat heart with potent hypotensive and natriuretic potency .
|
-
- HY-P1519
-
|
BNP (1-32), rat
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Brain Natriuretic Peptide (1-32), rat (BNP (1-32), rat) is a 32 amino acid polypeptide secreted by the ventricles of the heart in response to excessive stretching of heart muscle cells (cardiomyocytes) .
|
-
- HY-P3857
-
|
|
Peptides
|
Neurological Disease
|
|
Carassin is a 21 amino acid tachykinin-related peptide, it can be isolated from the goldfish brain. Carassin has moderate affinity for rat tachykinin binding sites .
|
-
- HY-P2457
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS .
|
-
- HY-P10268
-
|
|
Peptides
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide K, human, porcine, rat exhibits bioactivity in gallbladder contraction, protein extravasation, hypotension and brcnchial smooth muscle spasm. Neuropeptide K, human, porcine, rat is concentrated in brain and acts as tachykinin neuromessenger .
|
-
- HY-P1239
-
|
|
Peptides
|
Neurological Disease
|
|
Neuromedin S(rat) is a 34-amino acids peptide from rat Neuromedin S. Neuromedin S is a neuropeptide isolated from rat brain. Neuromedin S acts as a ligand for the G protein-coupled receptor FM4/TGR-1
|
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1239A
-
|
|
Peptides
|
Neurological Disease
|
|
Neuromedin S(rat) TFA is a 34-amino acids peptide from rat Neuromedin S. Neuromedin S is a neuropeptide isolated from rat brain. Neuromedin S acts as a ligand for the G protein-coupled receptor FM4/TGR-1
|
-
- HY-P2636
-
|
Prepro CCK Fragment V-9-M
|
Peptides
|
Metabolic Disease
|
|
Cholecystokinin Precursor (24-32) (rat) is a cholecystokinin precursor that can be expressed in the heart, lungs, and kidneys as well as in the gastrointestinal tract and brain. Cholecystokinin is a brain-gut peptide that stimulates gallbladder contraction and pancreatic exocrine secretion and also acts as a neurotransmitter .
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-
- HY-P1303
-
|
|
5-HT Receptor
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Neurological Disease
|
|
CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-P1303A
-
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-P3964
-
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Endogenous Metabolite
|
Endocrinology
|
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TRH Precursor Peptide is a precursor peptide of thyrotropin-releasing hormone (TRH). TRH Precursor Peptide formation of TRH in rat brain and pituitary is zinc-dependent .
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- HY-P1134
-
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5-HT Receptor
|
Neurological Disease
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Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
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-
- HY-148195
-
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Peptides
|
Neurological Disease
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NNZ 2591 is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). NNZ 2591 shows orally active and cross the blood-brain barrier. NNZ 2591 shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. NNZ 2591 has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-106224B
-
|
Hypocretin-1 (human, rat, mouse) (acetate)
|
Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .
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-
- HY-P10153
-
|
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Peptides
|
Others
|
|
gH625 is a cell-penetrating viral peptide which is a part of glycoprotein H of Herpes simplex virus type I. gH625 is able to cross the cell membrane and to transport many conjugated cargoes into the cytosol. gH625 is permeable to the blood-brain barrier (BBB) and can enter the rat brain in vivo without toxic effects. gH625 can be used for siRNA delivery research .
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-
- HY-P1238
-
|
Neuromedin U (rat); rat neuromedin U-23
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Peptides
|
Neurological Disease
|
|
Neuromedin U, rat is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.
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-
- HY-P1238A
-
|
Neuromedin U (rat) (TFA); rat neuromedin U-23 TFA
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Peptides
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Neurological Disease
|
|
Neuromedin U, rat TFA is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.
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-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
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-
- HY-P3071
-
|
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Inflammation/Immunology
|
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ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
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-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
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-
- HY-P2601A
-
|
|
Peptides
|
Others
|
|
Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM .
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-
- HY-P4052
-
|
|
ROS Kinase
|
Neurological Disease
|
|
Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygen species (ROS) accumulation and suppresses the activation of ERK 1/2. Pinealon stimulates the functional activity of the main cellular elements of brain tissue, reduces the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia .
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-
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
|
Others
Neurological Disease
Metabolic Disease
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
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-
- HY-P3883
-
-
- HY-P1318
-
|
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Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
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-
- HY-P5754B
-
|
|
Apoptosis
|
Neurological Disease
|
|
TAT-NEP1-40 acetate is a therapeutic candidate for axonal regeneration and functional recovery after stroke. TAT-NEP1-40 acetate can protect PC12 cells against oxygen and glucose deprivation (OGD) and promote neurite outgrowth. TAT-NEP1-40 acetate protects the brain against ischemia/reperfusion injury through inhibition of neuronal apoptosis. TAT-NEP1-40 acetate can be efficiently delivered into the rat brains .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0435
-
-
-
- HY-N2070
-
-
-
- HY-116663
-
-
-
- HY-N2080
-
-
-
- HY-N13258
-
-
-
- HY-100821
-
-
-
- HY-114651
-
-
-
- HY-113516
-
-
-
- HY-129665
-
-
-
- HY-126644
-
-
-
- HY-N2160
-
-
-
- HY-B1614
-
-
-
- HY-110016
-
-
-
- HY-N0745
-
-
-
- HY-113149
-
-
-
- HY-113149A
-
-
-
- HY-B1614R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Adrenergic Receptor
|
|
Clenbuterol (hydrochloride) (Standard) is the analytical standard of Clenbuterol (hydrochloride). This product is intended for research and analytical applications. Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .
|
-
-
- HY-126419
-
-
-
- HY-B0573
-
-
-
- HY-B0573B
-
-
-
- HY-N3807
-
-
-
- HY-B0573R
-
|
|
Alkaloids
Other Alkaloids
Source classification
Endogenous metabolite
|
Adrenergic Receptor
Bacterial
|
|
Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
|
-
-
- HY-N9480
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0573BS
-
|
|
|
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
-
- HY-B0573S
-
|
|
|
Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
-
- HY-B0573S1
-
|
|
|
Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
|
-
-
- HY-14280S
-
|
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
-
- HY-14605S
-
|
|
|
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylateis the deuterium labeledRasagiline (mesylate)(HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively .
|
-
-
- HY-A0168S
-
|
|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-131693A
-
|
GAG hydrochloride
|
|
Alkynes
|
|
γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA hydrochloride can increase the concentration of GABA in rat brain . γ-Acetylenic GABA (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14605
-
|
(R)-AGN1135 mesylate; TVP1012 mesylate
|
|
Alkynes
|
|
Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14605A
-
Rasagiline
Maximum Cited Publications
6 Publications Verification
(R)-AGN1135; TVP1012
|
|
Alkynes
|
|
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-14200
-
|
TVP1022; S-PAI
|
|
Alkynes
|
|
(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-131693
-
|
GAG
|
|
Alkynes
|
|
γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain . γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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![[Glp5,(Me)Phe8,Sar9] Substance P (5-11)](http://file.medchemexpress.eu/product_pic/hy-p3801.gif)
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