Neurological Disease

TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death.

Myristic acid-¹³C₂ is the ¹³C-labeled Myristic acid (HY-N2041). Myristic acid is an orally active saturated 14-carbon fatty acid found in most animal and plant fats, especially milk fat coconut oil, palm oil and nutmeg oil. Myristic acid exerts anti-inflammatory activity through the NF-κB pathway. Myristic acid has antibacterial, anti-inflammatory and analgesic properties.

3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC₅₀of 773 nM. Tolcapone can inhibits α-syn and Aβ₄₂ oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma.

JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC₅₀ of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats.

PDE10-IN-2 is a PDE10 inhibitor with an IC₅₀≦0.01 μM.

Benactyzine is a competitive BChE inhibitor with a K_i of 0.01 mM. Benactyzine is an anticholinergic drug. Benactyzine has the potential for organophosphate poisoning research.

DOI hydrochloride (Standard) is the analytical standard of DOI hydrochloride (HY-103124). This product is intended for research and analytical applications. DOI hydrochloride is a serotonin 5-HT2A/2C receptor agonist with K_i values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice.

Cismethrin is a pyrethroid insecticide that produces Type I effects on intact nerve.

Dipyanone hydrochloride is structurally similar to known opioids.

mNOX-E36 is a murine-specific analogue of NOX-E36 (HY-148100), an anti-CCL-2 L-RNA aptamer that binds and neutralises the mouse chemokine CCL-2. mNOX-E36 reduces scarring in an experimental murine model of glaucoma filtration surgery (GFS). mNOX-E36 ameliorates lupus nephritis in mice. mNOX-E36 can be used for GFS and lupus nephritis research.

5-Fluoro PB-22 N-(2-fluoropentyl) isomer is a derivative of cannabinoid.

Cavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain.

Teniloxazine free base is an inhibitor for norepinephrine neuronal reuptake and an weak inhibitor for reuptake of Serotonin (HY-B1473A) and Dopamine (HY-B0451). Teniloxazine free base exhibits antidepressant, antihypoxic and anti-amnestic properties without anticholinergic, sedative, and cardiovascular adverse effects.

Verubecestat tosylate is an orally active, high-affinity BACE1 and BACE2 inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease.

Facinicline hydrochloride (Standard) is the analytical standard of Facinicline (hydrochloride) (HY-108057A). This product is intended for research and analytical applications. Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K_i of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a K_i value of 1.2 nM.

Budipine (Standard) is the analytical standard of Budipine. This product is intended for research and analytical applications. Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease.

Ropinirole-d₄ (SKF 101468-d₄) hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a K_iof 29 nM for D2 receptor. Ropinirole hydrochloride has pEC₅₀s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.

Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .

IRL 1038 is an endothelin B receptor selective antagonist with a K_i of 6-11 nM.

VU0422288 (Standard) is the analytical standard of VU0422288 (HY-110190). This product is intended for research and analytical applications. VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC₅₀s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.