Neurological Disease

JB062 is a nonmuscle myosin inhibitor with IC₅₀ values of 1.6, 5.4, and >100 μM for Skeletal muscle myosin, Cardiac muscle myosin, and Smooth muscle myosin II, respectively. JB062 has cytotoxic to human cancer cells but not normal cells. JB062 can be used in research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research.

ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC₅₀ value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc.

β-Amyloid-¹⁵N (1-40) (TFA) is the ¹⁵N-labledβ-Amyloid (1-40) (TFA). β-Amyloid (1-40) is a primary protein in plaques found in the brains of patients with Alzheimer's disease.

SM 32 is an analgesic. SM 32 produces an increase in ACh release. SM 32 amplifies electrically- and nicotine- evoked guinea-pig ileum contractions. SM32 induces antinociceptive effects through a central cholinergic mechanism.

BDT001 (Example 1) is a selective FLT3 receptor antagonist that can be used in the research of pain disorders, cancer, and autoimmune diseases.

Chlorisondamine is a nicotinic antagonist that acts as a ganglionic blocker and has been utilized to evaluate the neurogenic contributions to blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine has demonstrated antihypertensive properties, primarily being assessed through its effects on blood pressure, cardiac output, and heart rate in various experimental settings, particularly in mice.

Bmapn has rewarding and reinforcing properties, decreases dopamine transporter and increases dopamine receptor D2 gene expression in the striatum.

Cy3 labled Rovanersen sodium is a Cy3 labled Rovanersen sodium.

Moxonidine-d₇ is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I₁-R) agonist. Moxonidine activates imidazoline I₁ receptors and α₂ adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.

GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD.

AChE-IN-30 is an AChE inhibitor with an IC₅₀ value of 4.4 μM. AChE-IN-30 has neuroprotective activity, and inhibits H₂O₂-induced apoptosis by suppressing intracellular ROS accumulation. AChE-IN-30 can be used for research of Alzheimer's disease.

Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABA_A receptors and NaV_1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED₅₀ of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC₅₀ of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable.

Muscarinic M3 receptor antagonist-2 (Compound 30) is a muscarinic M3 receptor antagonist.

Propizepine is a tricyclic antidepressant compound.

Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 is a multi-opioid receptor (Opioid Receptor) modulator, acting as a MOR/KOR agonist and a DOR antagonist. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 activates the G protein-mediated cAMP inhibitory pathway and β-arrestin2 recruitment pathway downstream of MOR, with an EC₅₀ of 159 nM for β-arrestin2 recruitment, an EC₅₀ of 1.1 nM for MOR-mediated calcium mobilization, and an EC₅₀ of 397 nM for KOR. Tyr-c [D-Lys-p-F-Phe-Phe-Asp]-D-Pro-NH2 exhibits potent analgesic activity in vivo. It can be used in studies related to opioid receptor function and analgesia.

Gabapentin-d₆ (hydrochloride) is deuterium labeled Gabapentin (hydrochloride).

PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC₅₀ of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury.

Maxi-K modulator 1 (Example 1) is a Maximum conductance calcium-activated potassium (Maxi-K) channel modulator. Maxi-K modulator 1 has a potent stimulating effect on Maxi-K channel activity. Maxi-K modulator 1 can be used for fragile X syndrome research.

Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM).