Neurological Disease

Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC₅₀: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models.

5-HT₇R antagonist 3 (Compound 6.4) is a selective 5-HT₇R antagonist (K_i: 8 nM), with K_i of 511 nM (D₂), 8930 nM (5-HT_1A) and 5786 nM (5-HT_2A), respectively. 5-HT₇R antagonist 3 possesses antidepressant and anxiolytic effects in mice.

Levinoid C is a Cytochrome P450-modified bacterial terpenoid. Levinoid C shows moderate neuroprotective activity against glutamate-induced excitotoxicity cell model with an EC₅₀ of 21 μM.

Eslicarbazepine-d₃ (BIA 2-194-d₃) is the deuterium labeled Eslicarbazepine (HY-114703). Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.

RIPK1-IN-21 (Compound I-5) is an inhibitor of RIPK1 with an EC₅₀ value of 14.8 nM. RIPK1-IN-21 can be used in the research of neurodegenerative, autoimmune, and inflammatory diseases.

Roflurane (DA 893) is a halocarbon agent that can relieve pain.

P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC₅₀ values of 4.2 nM in humans and 6.8 nM in rats.

Meldonium (dihydrate) (Standard) is the analytical standard of Meldonium (dihydrate). This product is intended for research and analytical applications. Meldonium (MET-88) dihydrate functions as a cardioprotective agent by cpmpetetively inhibiting γ-butyrobetaine hydroxylase (BBOX) and carnitine/organic cation transporter type 2 (OCTN2). Mildronate dihydrate exhibits IC₅₀ values of 34-62 μM for human recombinant BBOX and an EC₅₀ of 21 μM for human OCTN2. Meldonium dihydrate is a fatty acid oxidation inhibitor.

Sintropium bromide is a mAChR antagonist with anticholinergic effects. Sintropium bromide can be used for pain and spasm research.

CXT29 is an orally active COX-2 inhibitor and a thromboxane A₂ receptor (TP) antagonist. CXT29 exhibits COX inhibitory activity and selectivity, with IC₅₀ values of 13 and 722 nM for COX-2 and COX-1 respectively. CXT29 inhibits platelet aggregation induced by U-46619 (HY-108566) (a TP agonist), with an IC₅₀ of 96 nM. CXT29 effectively inhibits the production of TXB₂ and PGE₂, significantly reducing platelet aggregation and inflammatory pain in mice. CXT29 can be used for research on inflammatory pain and cardiovascular diseases.

SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs.

MAGL-IN-13 (compound (3R, 4S) - 5v) is a selective, irreversible inhibitor for MAGL,with IC₅₀ values of 0.026, 0.021 and 0.24 nM for mMAGL, hMAGL and rMAGL, respectively. MAGL-IN-13 can penetrant blood brain barrier. .

2-(Phenylethynyl)-ATP (ammonium) is a selective and potent GPR17 agonist with an EC₅₀ of 35 pM. 2-(Phenylethynyl)-ATP (ammonium) also shows weak activation of P2Y Receptor. 2-(Phenylethynyl)-ATP (ammonium) can be used for the research of neurological disease.

Dichlorphenamide (Diclofenamide) disodium is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research.

Ferroptosis-IN-17 (Compound 18) is a ferroptosis (Ferroptosis) inhibitor with an EC₅₀ value of 0.57 μM. Ferroptosis-IN-17 reduces intracellular ferrous ion accumulation, lipid peroxidation, and effectively restores the levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). Ferroptosis-IN-17 shows good solubility and significant metabolic stability in rat plasma. Ferroptosis-IN-17 is promising for research in tumor suppression, neurodegenerative diseases, and cardiovascular diseases.

HDAC6-IN-52 (EX.1) is a potent inhibitor of HDAC6, with the inhibitory rate of 100% at 10 μM. HDAC6-IN-52 plays an important role in central nervous system diseases including neurodegenerative diseases such as Alzheimer’s disease andprogressive supranuclear palsy.

Lemairamin (Wgx-50) is a hydroxylamine compound. Lemairamin can be isolated from the pericarps of the Zanthoxylum plants. Lemairamin activates α7nAChR, stimulates the expression of IL-10 and POMC. Lemairamin shows a decrease in Akt. Lemairamin attenuates DSS-induced intestinal inflammation. Lemairamin alleviates pain hypersensitivity.

TIPP is a potent and selective δ-opioid antagonist with a K_i value of 1.22 nM.

β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.

Acetylcysteine-¹⁵N (N-Acetylcysteine-¹⁵N) is the ¹⁵N-labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine is the most stable form of cysteine during drug delivery and can be used in disulfidptosis studies.