Neurological Disease

Muscarine ((+)-Muscarine) chloride is an agonist of prototype mAChR. Muscarine chloride is a toxin that can stimulate the parasympathetic nervous system.

Adrenochrome (Adraxone) is an oxidation product of Epinephrine. Adrenochrome is a potent coronary constricting agent in the rat heart. Adrenochrome can be used for neurological disorder research.

Alizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders.

NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC₅₀s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression.

Tetracosactide acetate (Tetracosactrin acetate ) is the acetate salt form of Tetracosactide (HY-P0060). Tetracosactide acetate is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide acetate is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC₅₀ of 0.65 nM. Tetracosactide acetate can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide acetate is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.

AMPA-IN-3 is an AMPA receptor inhibitor. AMPA-IN-3 inhibits TARP J2-dependent AMPA receptor activity with a pIC₅₀ value of 10.7. A AMPA-IN-3 can be used for the research of neurological disease.

(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with K_i values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.

pan-HCN-IN-1 is a potent HCN ion channel inhibitor with IC₅₀ values of 58 nM, 522 nM, 58 nM, and 58 nM against HCN1, HCN2, HCN3, and HCN4, respectively. pan-HCN-IN-1 exerts voltage-dependent but not use-dependent inhibition, potently inhibits channels in the closed state, and significantly slows the activation time constant of HCN1 currents. pan-HCN-IN-1 can be used for the research of cognitive dysfunction.

Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT_1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT_1A (IC₅₀=0.9 nM). Antipsychotic and antidepressant activities.

DB-3-291 is a CSK-targeting agent with a human CSK K_d of 1 nM and high selectivity for CSK over other kinases bound by dasatinib. DB-3-291 induces targeted degradation of CSK via a ubiquitin-dependent pathway and incorporates dasatinib as the kinase binding ligand. DB-3-291 can be used for the research of innate immune responses to viral DNA.

Glycine-¹³C₂,¹⁵N is the ¹³C- and ¹⁵N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.

2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances.

CP 93129 dihydrochloride is a potent 5HT_1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.

Obtusin is an orally active human monoamine oxidase A (hMAO-A) inhibitor discovered from the seeds of Cassia obtusifolia, with a K_i value of 6.15 μM. Obtusin inhibits high glucose-induced activation of the MAPKs/NF-κB/VEGF pathway and downregulates the expression of Poldip2, Nox4, VCAM-1, and HIF-1α, thereby alleviating oxidative stress, endothelial activation, and angiogenesis-related functions. Obtusin ameliorates diabetic retinopathy in vivo. Obtusin is used in research related to diabetes and neurodegenerative diseases (anxiety and depression).

SC 51089 free base is a selective antagonist of prostaglandin E₂ EP1 receptor, with K_is of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.

Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable.

5-Hydroxyindole-3-acetic acid-d₂ is the deuterium labeled 5-Hydroxyindole-3-acetic acid. 5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.

Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC₅₀ as low as 17 nM against human HDAC6. Bavarostat can be labeled with ¹⁸F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers.

Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca²⁺-dependent K⁺ channel.