Neurological Disease

Rivastigmine-d₄ (tartrate) is deuterium labeled Rivastigmine (tartrate). Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC₅₀s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.

Gelsemine (Standard) is the analytical standard of Gelsemine. This product is intended for research and analytical applications. Gelsemine, an alkaloid from the Chinese herb Gelsemium elegans, is effective in mitigating chronic pain. Antinociceptive effects.

U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC₅₀ of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic.

Spiperone (Standard) is the analytical standard of Spiperone. This product is intended for research and analytical applications. Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.

Alniditan (Alnitidan) is a potent 5-HT_1B and 5-HT_1D receptors agonist, with IC₅₀s of 1.7 nM and 1.3 nM for h5-HT_1B and h5-HT_1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects.

MAFP (Standard) is the analytical standard of MAFP (HY-103334). This product is intended for research and analytical applications. MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

PF-04701475 is a potent AMPA receptor potentiator with an EC₅₀ of 123 nM. PF-04701475 can be used for the study of neurological disorders.

VER-155008 (Standard) is the analytical standard of VER-155008 (HY-10941). This product is intended for research and analytical applications. VER-155008 is an inhibitor of Hsp70, with IC₅₀s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a K_d of 0.3 μM for Hsp70.

NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia.

PF 04531083 (Standard) is the analytical standard of PF 04531083 (HY-105283). This product is intended for research and analytical applications. PF 04531083 is an orally active and selective NaV1.8 blocker with an IC₅₀ of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain.

Vigabatrin (hydrochloride) (Standard) is the analytical standard of Vigabatrin (hydrochloride). This product is intended for research and analytical applications. Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.

JNJ-47965567 (Standard) is the analytical standard of JNJ-47965567 (HY-101418). This product is intended for research and analytical applications. JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.

ABT-670 is a selective, oral bioavailable agonist of dopamine D₄ receptor, with EC₅₀ of 89 nM, 160 nM, and 93 nM for human D₄, ferret D₄, and rat D₄, respectively.

Sp-cAMPS (sodium salt) (Standard) is the analytical standard of Sp-cAMPS (sodium salt) (HY-100530C). This product is intended for research and analytical applications. Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.

Tiagabine-d₆ (NO050328-d₆) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

2-(Phosphonooxy)benzoic acid is a non-acetylated salicylic acid derivative which has the potential for inflammatory disease as well as in analgesic therapy.

Nafimidone alcohol is the major metabolic of Nafimidone in plasma and urine. Nafimidone alcohol is promising for research of onset seizures.

BN80933 is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a rat K_i of 0.92 μM. BN80933 inhibits lipid peroxidation, and blocks hypoxia-induced lactate dehydrogenase elevation and delayed 8-epiprostaglandin F₂α elevation. BN80933 can be used for the research of stroke, and traumatic brain injury.

PB-22 5-hydroxyquinoline isomer is a structural isomer of PB-22. PB-22 is a cannabinoid.

LY2811376 (Standard) is the analytical standard of LY2811376 (HY-10472). This product is intended for research and analytical applications. LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC₅₀ of 239 nM-249 nM, that acts to decrease Aβ secretion with EC₅₀ of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.