Neurological Disease

PaPE-1 is a pathway-preferential estrogen receptor (ER) agonist that preferentially activates ER non-nuclear-initiated signaling while minimally activating nuclear-initiated signaling. PaPE-1 exhibits K_i values of 10 μM and 25 μM for human ERα and ERβ, respectively. The relatively low ER affinity and rapid receptor dissociation of PaPE-1 facilitate the triggering of non-nuclear mTOR/MAPK/AKT signaling, while reducing the recruitment of ERα to chromatin and sustained nuclear ER-dependent transcription. PaPE-1 is suitable for research related to non-nuclear ER signaling, metabolic disorders, ischemic brain injury, Alzheimer's disease, and ER-positive breast cancer.

25H-NBOH hydrochloride is a phenethylamine.

FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex.

Pargolol hydrochloride is a β adrenergic receptor antagonist. Pargolol 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.

AGN-201781 is an orally active α-2B adrenergic receptor agonist. AGN-201781 can be used in studies related to neuropathic pain.

Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders.

BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury.

SYM 2081 (Standard) is the analytical standard of SYM 2081 (HY-101310). This product is intended for research and analytical applications. SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.

Sacubitrilat-¹³C₄ (Desethyl Sacubitril-¹³C₄) is ¹³C labeled Sacubitrilat. Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

C18:0 GM1-biotin (ammonium) is a biotin labled ganglioside.

Asenapine-d₃,¹³C (Org 5222-d₃,¹³C) is deuterium and ¹³C labeled Asenapine. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.

Imagabalin (PD-0332334 free base) is an active compound with activity for studying neurological diseases. The synthesis of imagabalin involves the reaction of 3-methylvaleric acid and Meldrum acid. During the synthesis of imagabalin, an acyl chloride intermediate species, 3-methylvaleryl chloride, was revealed for the first time. The synthesis of imagabalin also provided new information about the reaction mechanism, indicating that 3-methylvaleric anhydride is an important intermediate.

NS11394 (Standard) is the analytical standard of NS11394 (HY-11048). This product is intended for research and analytical applications. NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.

Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1).

Ephenidine hydrochloride is structurally categorized as a phenethylamine.

Teneligliptin-d₅ (MP-513-d₅) is deuterium labeled Teneligliptin. Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC₅₀s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.

PiPT is a Tryptamine (HY-B2132) compound.

GSK-3β inhibitor 26 (Compound D14) is a GSK-3β inhibitor with an IC₅₀ of 18.23 μM. GSK-3β inhibitor 26 can be used in the research of cancer, inflammation and neurodegenerative diseases.

BP 897 hydrochloride (Standard) is the analytical standard of BP 897 (hydrochloride) (HY-106660). This product is intended for research and analytical applications. BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (K_i=0.92 nM) and a 70 times lower affinity at the D2 receptor (K_i=61 nM).

Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.