Neurological Disease

ROCK-IN-13 is a ROCK2 inhibitor with an IC₅₀ of 8 nM against human ROCK2. ROCK-IN-13 has the potential for use in the research of diseases such as multiple sclerosis, glaucoma, and cardiovascular diseases.

AZ-PFKFB3-67 (Standard) is the analytical standard of AZ-PFKFB3-67 (HY-101972). This product is intended for research and analytical applications. AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC₅₀s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity.

SFRP1 modulator-1 (compound Way 316606 (positive control)) is a SFRP1 modulator.

Mexiletine-d₃ (KOE-1173-d₃) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC₅₀ : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research.

UNC11676A is an MDA5 ATPase inhibitor with IC₅₀ values of 6 μM, 115 μM and 108 μM against MDA5, LGP2 and DDX1, respectively. MDA5, LGP2 and DDX1 are three human DExD/H-box RNA helicases. UNC11676A can be used in the research of Aicardi-Goutières syndrome, Singleton-Merten syndrome, systemic lupus erythematosus and Alzheimer's disease.

Lisuride maleate (Standard) is the analytical standard of Lisuride (maleate) (HY-110080). This product is intended for research and analytical applications. Lisuride (maleate) is a potent agonist of dopamine with a probably direct action on dopaminergic receptors. Lisuride (maleate) is an ergot derivative. Lisuride (maleate) releases the premenstrual mastalgia without significant side effects.

Riluzole hydrochloride (Standard) is the analytical standard of Riluzole hydrochloride. This product is intended for research and analytical applications. Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

Pentiapine (Standard) is the analytical standard of Pentiapine (HY-100143). This product is intended for research and analytical applications. Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites.

Ru-32514 is an agonist of benzodiazepine receptor.

Pipoxolan is an orally active smooth muscle relaxant, anti-inflammatory agent and anticancer agent. Pipoxolan modulates PI3K/AKT signaling pathways, and reduces the levels of Ras/MEK/p-ERK, MMP-2 and MMP-9. Pipoxolan inhibits pro-inflammatory transcription factor pathways, activates Nrf2/HO-1, and suppresses the production of pro-inflammatory mediators. Pipoxolan induces ROS generation, endogenous mitochondrial Apoptosis, and G₀/G₁ cell cycle arrest. Pipoxolan reduces cerebral infarction size and inhibits intimal hyperplasia. Pipoxolan can be used in research related to cerebral ischemia, intimal hyperplasia, oral squamous cell carcinoma, leukemia and lung cancer.

Ropinirole (hydrochloride) (Standard) is the analytical standard of Ropinirole (hydrochloride). This product is intended for research and analytical applications. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D₃/D₂ receptor agonist with a K_i of 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.

GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder.

SBI-0206965 (Standard) is the analytical standard of SBI-0206965 (HY-16966). This product is intended for research and analytical applications. SBI-0206965 is a potent, selective and cell permeable autophagy K_inase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 K_inase and 711 nM for the highly related K_inase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.

Mebeverine acid-d₃ (Mebeverine metabolite Mebeverine acid-d₃) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.

Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.

Sigma ligand-1 (Standard) is the analytical standard of Sigma ligand-1 (HY-101626). This product is intended for research and analytical applications. Sigma ligand-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 has a Ki of 4000 nM at the dopamine D2 receptor.

5-APDI hydrochloride is an indane with an amphetamine-like aminopropane group. 5-APDI hydrochloride inhibits the uptake of serotonin, dopamine, and norepinephrine by crude synaptosomes (IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively).

Zegocractin (Standard) is the analytical standard of Zegocractin (HY-101942). This product is intended for research and analytical applications. Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC₅₀s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

Emrusolmin (Standard) (Anle138b (Standard)) is the analytical standard of Emrusolmin (HY-101855). This product is intended for research and analytical applications. Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.

Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC₅₀ of 6.8 μM.