Ischemic Stroke

Lifarizine is a sodium channel blocker with neuroprotective properties.

ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca²⁺ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.

Ganoderic acid K is a triterpenoid compound. Ganoderic acid K can be isolated from Ganoderma lucidum. Ganoderic acid K inhibits ACE activity with an IC₅₀ of 2.6×10^-5 M. Ganoderic acid K exhibits direct, high-affinity binding to recombinant MD2 protein, with a K_d value of 0.47 μM. It potently inhibits LPS-induced release of TNF-α and IL-6. It reduces cerebral infarction volume and ameliorates neurological dysfunction in mice with ischemic stroke in the tMCAO model. Ganoderic acid K can be used in studies related to hypertension and ischemic stroke.

PaPE-1 is a pathway-preferential estrogen receptor (ER) agonist that preferentially activates ER non-nuclear-initiated signaling while minimally activating nuclear-initiated signaling. PaPE-1 exhibits K_i values of 10 μM and 25 μM for human ERα and ERβ, respectively. The relatively low ER affinity and rapid receptor dissociation of PaPE-1 facilitate the triggering of non-nuclear mTOR/MAPK/AKT signaling, while reducing the recruitment of ERα to chromatin and sustained nuclear ER-dependent transcription. PaPE-1 is suitable for research related to non-nuclear ER signaling, metabolic disorders, ischemic brain injury, Alzheimer's disease, and ER-positive breast cancer.

Anticonvulsant agent 12 is a naphthalene-containing azole compound with anticonvulsant activity. Anticonvulsant agent 12 can be used in the research of central nervous system diseases including anxiety, depression, convulsion, epilepsy, migraine, bipolar disorder, substance abuse, smoking, ADHD, obesity, sleep disorders, stroke, neuropathic pain, cognitive impairment, neurodegenerative diseases and muscle spasms.

Dioxadrol is an uncompetitive NMDA receptor (PCP binding site) antagonist, with a K_i value of 10.9 nM in pigs. Dioxadrol binds to the phencyclidine (PCP) binding site within the cation channel associated with the NMDA receptor, thereby blocking cation influx. Dioxadrol possesses local anesthetic, spasmolytic and central nervous system activities, including phencyclidine-like dissociative anesthetic properties. Dioxadrol can be used in the research of Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-associated dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, ischemic stroke, central nervous system trauma, and epilepsy.

B-Raf-IN-21 is a B-Raf kinase inhibitor with a K_d of 4.8 nM and an IC₅₀ of 6 nM. B-Raf-IN-21 can be used for the research of stroke.

BN80933 is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a rat K_i of 0.92 μM. BN80933 inhibits lipid peroxidation, and blocks hypoxia-induced lactate dehydrogenase elevation and delayed 8-epiprostaglandin F₂α elevation. BN80933 can be used for the research of stroke, and traumatic brain injury.

(Rac)-BW 245C is a Rac isomer of BW 245C (HY-101987 ). BW 245C is a prostanoid DP-receptor (DP1) agonist, can be used to study stroke.

Norfluoxetine oxalate is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine oxalate exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine oxalate inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine oxalate can be used in research related to depression, ischemic stroke, and epilepsy.

2'-Acetylacteoside (Standard) is the analytical standard of 2'-Acetylacteoside (2'-AA) (HY-N0026). This product is intended for research and analytical applications. 2'-Acetylacteoside is a natural compound with oral activity and blood-brain barrier permeability. 2'-Acetylacteosideexhibits MAO‑B inhibitory activity (IC₅₀ = 17.71 μM, K_i = 13.81 μM). 2'-Acetylacteoside downregulates the expression of RANK, TRAF6, NF‑κB, NFATc1 and IKKβ, disrupts the RANKL/RANK interaction, blocks downstream signaling pathways, and increases the level of phosphorylated Akt. 2'-Acetylacteoside possesses potent anti-osteoclastogenic, anti-bone resorptive, pro-neurogenic, neuroprotective and antioxidant activities. 2'-Acetylacteoside can be used in the research of osteoporosis, ischemic stroke and Parkinson's disease.

TPT-260 (TPU260), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (K_d = ~5 µM). TPT-260 increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease.