Neurological Disease

Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT₄R), with a pK_i of 7.7. Velusetrag hydrochloride exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease.

Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT_1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT_1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT₂ and the α₁-adrenergic function.

3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABA_A receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.

Eprobemide is a non-competitive reversible inhibitor of monoamine oxidase A.

(S)-SCH-23390 hydrochloride is the S-enantiomer of SCH-23390 (HY-19545). SCH-23390 is a dopamine D1-like receptor antagonist (with K_i values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively).

CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC₅₀=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction.

GW542573X is a potent and selective Ca²⁺-activated K⁺ 2 (SK2) channels activator. GW542573X induces the Ca²⁺-response curve of hSK1 that left-shifted from an EC₅₀ (Ca²⁺) value of 410 nM to 240 nM.

TRPM8 agonist WS-3 is an specific agonist of TRPM8 with an EC₅₀ of 3.7 μM. TRPM8 agonist WS-3 inhibits epileptic seizures through a TRPM8 dependent mechanism. TRPM8 agonist WS-3 can be used for research on epilepsy and other conditions.

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 .

AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders, such as vascular dementia (VaD).

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.

Benzoin (DL-Benzoin) is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116).

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.

L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC₅₀: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test.

SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC₅₀=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.

Bepridil (CERM 1978 (free base); Org 5730) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Bupivacaine (hydrochloride) (Standard) is the analytical standard of Bupivacaine (hydrochloride). This product is intended for research and analytical applications. Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.

Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC₅₀s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices. Nrf2-ARE/hMAO-B/QR2 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Procaine (hydrochloride) (Standard) is the analytical standard of Procaine (hydrochloride). This product is intended for research and analytical applications. Procaine hydrochloride is a DNA-demethylating agent. Procaine hydrochloride acts through multiple targets and has a slow onset and a short duration of action.

Ceruloplasmin is a copper-containing multifunctional ferrous oxidase glycoprotein. Ceruloplasmin specifically oxidizes Fe²⁺ to Fe³⁺, promoting the binding of Fe³⁺ to transferrin. Ceruloplasmin can bind to copper ions to prevent the toxicity of free copper to cells. Ceruloplasmin can be used for the research of inflammation, metabolic and neurological disease such as Parkinson’s disease.