Neurological Disease

(S)-(+)-O-Desmethyl Venlafaxine is a S-enantiomer of O-Desmethyl Venlafaxine. O-Desmethyl Venlafaxine is an active metabolite of Venlafaxine. Venlafaxine (HY-B0196) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.

P2X3 antagonist 39 (compound 26a) is a selective P2X3 receptor antagonist with an IC₅₀ value of 54.9 nM. P2X3 antagonist 39 can be used in the study of neuropathic pain model.

BRP-821 is a soluble epoxide hydrolase (sEH) inhibitor with an IC₅₀ of 0.4 nM. BRP-821 can be used for the researches of inflammation, cardiovascular, metabolic and neurological disease .

Nocistatin (Bovine) is a nociceptin precursor contains another biologically active peptide. Nocistatin (Bovine) blocks nociception-induced allodynia and hyperalgesia. Nocistatin (Bovine) also attenuates pain evoked by prostaglandin E2. Nocistatin (Bovine) can bind to the membrane of mouse brain and spinal cord with high affinity. Nocistatin (Bovine) can be studied in research on pain transmission.

(-)-Securinine nitrate is an alkaloid and also a GABA_A receptor antagonist. (-)-Securinine nitrate can be derived from plants.

Promethazine-d₃ (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.

NS4591 is a modulator of calcium-activated potassium channels with activity that enhances small (SK) and intermediate (IK) conductivity. NS4591 doubled IK-mediated currents in whole-cell patch-clamp experiments at a concentration of 45 +/- 6 nM, and doubled SK3-mediated currents at a concentration of 530 +/- 100 nM. NS4591 inhibits the number of action potentials generated by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons. NS4591 also reduced carbakol-induced detrusor ring contraction in the rat bladder, demonstrating sensitivity to apamin.

Meclofenoxate (Centrophenoxine) is an ester synthesized from DMAE and pCPA, which has the activity of stimulating memory and improving cognition.

(±)-Meclonazepam ((±)-Ro 11-3128) is the racemate of Meclonazepam (HY-101725). Meclonazepam (Ro 11-3128) is a benzodiazepine compound with anxiolytic effect. Meclonazepam exhibits antischistosomal activity against S. mansoni.

5-HT6R antagonist 5 (compound 1.2.12(4)) is a potent competitive 5-HT6R antagonist with an IC₅₀ of 4.19 nM. 5-HT6R antagonist 5 can be used for research in various central nervous system (CNS) diseases, cognitive and neurodegenerative diseases.

Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (K_is of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.

Carbromal (Standard) is the analytical standard of Carbromal. This product is intended for research and analytical applications. Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects.

Propoxur-d₃ is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

JNK-IN-22 (Compound 58) is a JNK-1 inhibitor.

HDAC degrader-2 is a HDAC degrader, and its DC₅₀ for HDAC1 in MM.1S cells is 2.55 μM. HDAC degrader-2 recruits and covalently binds to DDB1, thereby inducing proteasomal degradation of HDAC1 and HDAC2. HDAC degrader-2 inhibits HDAC6 activity and increases the acetylation levels of α-tubulin and histone H3. HDAC degrader-2 induces early and late apoptosis and reduces the proliferative capacity of cancer cells. HDAC degrader-2 can be used for research on multiple myeloma and breast cancer.

PyP-1 is a highly selective and potent PDE10 inhibitor. PyP-1 has a strong inhibitory effect on human PDE10A2 enzyme (K_i = 0.32 nM). PyP-1 can improve cognitive behavior. PyP-1 commonly used in research on conditions such as schizophrenia and cognitive impairment.

sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD).

ADN-138 is an aldose reductase inhibitor. ADN-138 reduces sorbitol levels in diabetic nerves and results in significant increases in MNCV and Na⁺, K⁺-ATPase in the nerves. ADN-138 can be used in the research of diabetic nerve complications.

YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a K_i of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC₅₀ of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.

AChE-IN-112 is an acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 0.41 μM. AChE-IN-112 scavenges various reactive oxygen and reactive nitrogen species, including DPPH, ABTS, NO, hydroxyl and hydrogen peroxide free radicals. AChE-IN-112 can be used for the research of Alzheimer's disease.