Neurological Disease

Antiarol (3,4,5-Trimethoxyphenol) is a phenolic compound present in the trunk of Coffea canephora. Antiarol is a metabolite produced by chicken cecal microbes, whose cecal content changes dynamically with the severity of wooden breast (WB; a muscle disease prevalent in broilers) and enters the plasma through circulation.

AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .

LE 300 is a potent and selective dopamine D1-like receptor antagonist with K_is of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT_2A receptor with a pA2 of 8.32 in a rat tail artery assay.

GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).

Murine Fibrinogen is a native fibrinogen derived from mouse plasma. Murine Fibrinogen acts as a cerebrovascular permeability enhancer. Murine Fibrinogen activates matrix metalloproteinase-9 (MMP-9), downregulates the expression of vascular endothelial cadherin (VE-cadherin), and upregulates the expression of plasmalemmal vesicle-associated protein-1 (PV-1). Murine Fibrinogen increases macromolecular leakage from pial veins, thereby disrupting the microvascular integrity of cerebral blood vessels. Murine Fibrinogen can be used in studies related to cerebrovascular dysfunction.

Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the K_i values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.

Brevetoxin B (Brevetoxin-2) is a red tide toxin. Brevetoxin B affects sodium, potassium and calcium currents in nerve terminals. Brevetoxin B also modulates the metabolic activity of Jurkat cells, reduces cell viability and induces apoptosis. Brevetoxin B can be used in research on synaptic transmission and tumors.

KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC₅₀ of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC₅₀=57.8 nM) and CLK3 (IC₅₀=488 nM).

CZL80, a brain-penetrable caspase-1 inhibitor with an IC₅₀ of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility.

Brexpiprazole-d₈ (OPC-34712-d₈) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM)^.

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC₅₀=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. Antinociceptive effect.

Corydine is a HIV-1 reverse transcriptase inhibitor and μ-opioid receptor (MOR) agonist, with an IC₅₀ of 356.7 μg/mL against HIV-1 reverse transcriptase, an EC₅₀ of 0.51 μM for MOR, and a K_i of 2.82 μM for MOR. Corydine produces antinociceptive effects by inhibiting acetic acid-induced writhing behavior in a MOR-dependent manner. Corydine inhibits the proliferation of cancer cells, mitogen-stimulated lymphocytes and IL-2-dependent cells. Corydine can be used in studies related to human immunodeficiency virus infection, visceral pain, leukemia, melanoma, bladder cancer and colon adenocarcinoma.

Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.

Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy.

Methsuximide (Mesuximide) is an orally active succinimide-derived antiepileptic agent. Methsuximide interacts with cytochrome P-450, increases the level of hepatic microsomal cytochrome P-450, and inhibits or competes with the cytochrome P-450 CYP 2C9/10 subtype. Methsuximide can be used in epilepsy-related research.

Nicotinamide-¹³C₆ is the ¹³C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.

CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity.

Palmitoyl glutamic acid (N-Palmitoyl-L-glutamic acid) is an acyl amino acid with neuroprotective effects. Palmitoyl glutamic acid is used as cosmetic material.

10(Z)-Pentadecenoic acid (cis-10-Pentadecenoic acid) is a monounsaturated fatty acid with Z configuration. 10(Z)-Pentadecenoic acid is degraded via two pathways, reductase-isomerase and epimerase. 10(Z)-Pentadecenoic acid is one of the major monounsaturated FAME components evaluated as biodiesel feedstock in Chlorella sp. RCS2. 10(Z)-Pentadecenoic acid weakly inhibits IFN-γ-induced IDO-1 activity and kynurenine production. 10(Z)-Pentadecenoic acid is a non-esterified fatty acid downregulated in adolescent depression and has diagnostic discriminatory potential. 10(Z)-Pentadecenoic acid is used in studies related to depression, inflammation, and lipid metabolism.

(±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC₅₀ value of 0.3 mM. (±)-Coniine hydrochloride shows acute toxicity with an LD₅₀ value of 7.7 mg/kg.