Neurological Disease

Chlothymol is a potent positive modulator of the GABA_A receptor subunit LGC-37, anticonvulsant, and antibacterial agent. Chlothymol inhibits Pentylenetetrazol-induced c-fos expression. Chlothymol inhibits the growth of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) strains, including LAC, with an MIC of 32 μg/mL. Chlorothymol has protective effects against epileptic seizures in various mouse models.

5-HT2A antagonist 4 methanesulfonate (Example 29) is a dopamine D2 receptor and serotonin 5HT2A receptor antagonist. 5-HT2A antagonist 4 methanesulfonate can be used for the study of central nervous system diseases.

Dehydroaripiprazole-d₈ is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.

Triflubazam is an anti-anxiety agent. Triflubazam can be used for the research of sleep disorder.

SB-334867 (Standard) is the analytical standard of SB-334867. This product is intended for research and analytical applications. SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

Pridopidine (Standard) is the analytical standard of Pridopidine. This product is intended for research and analytical applications. Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.

ABT-724 trihydrochloride (Standard) is the analytical standard of ABT-724 trihydrochloride (HY-103409). This product is intended for research and analytical applications. ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC₅₀ of 14.3 nM) and the ferret D4 receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC₅₀ values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively.

Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active.

Ripasudil (Standard) is the analytical standard of Ripasudil. This product is intended for research and analytical applications. Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.

5-Hydroxymethylcytosine-¹³C,d₂ is the ¹³C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes).

(S)-(+)-Carvone (Standard) is the analytical standard of (S)-(+)-Carvone. This product is intended for research and analytical applications. (S)-(+)-Carvone is an orally active natural product. (S)-(+)-Carvone increases the activity of antioxidant enzymes (SOD, CAT) and ROS, reduces the levels of oxidative stress markers (MDA, AChE), reduces the secretion of proinflammatory cytokines (IL-1β, IL-4, IL-6, IL-10), and downregulates NLRP3. (S)-(+)-Carvone increases the activities of caspase-8, -9 and -3. (S)-(+)-Carvone induces apoptotic death. (S)-(+)-Carvone has antimanic-like effect, liver protection and anticancer activity against skin cancer. (S)-(+)-Carvone improves memory and arthritis.

CP 53631 is an autophagy inhibitor (Autophagy) with anticancer activity. Additionally, CP 53631 can be used as an internal standard for Sertraline (HY-B0176A) in research related to selective serotonin reuptake inhibitors (SSRIs) in the field of antidepressants .

Alvelestat hydrochloride (AZD9668 hydrochloride) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat hydrochloride reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat hydrochloride restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat hydrochloride prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat hydrochloride inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat hydrochloride can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis.

Allylescaline hydrochloride is a derivative of the phenethylamine Escaline in which an allyl group replaces the ethyl group.

UPF-648 sodium salt is an effective inhibitor of kynurenine 3-monooxygenase (KMO), achieving approximately 81% inhibition at a concentration of 1uM, with no inhibitory effect on kynurenine aminotransferase (KAT).

Nefazodone (hydrochloride) (Standard) is the analytical standard of Nefazodone (hydrochloride). This product is intended for research and analytical applications. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.

Netupitant hydrochloride (CID 6451149 hydrochloride) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a K_i of 0.95 nM (CHO cells) against the human receptor. Netupitant hydrochloride antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant hydrochloride reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant hydrochloride can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression.

SD-1077 is a selectively deuterated precursor of dopamine (DA). SD-1077 can be used for the study of Parkinson's disease.