Neurological Disease

Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.

L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.

L-NAME hydrochloride inhibits NOS with an IC₅₀ of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC₅₀ value of 1.4 μM. L-NAME hydrochloride requires hydrolysis of the methyl ester by cellular esterases to become a fully functional inhibitor. L-NAME hydrochloride can be used to induce hypertension and preeclampsia models.

PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC₅₀=0.016 μM; K_i=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 is an ideal choose for microglia function research in healthy or diseased states. PLX5622 has been verified by MedChemExpress, which demonstrates desirable microglia depletion efficiency in mice. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm.

Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures.

L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases. L-Glutamic acid acts at ionotropic and metabotropic glutamate receptors.

Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.

α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC).

Substance P (Neurokinin P) is a CNS-penetrant neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

Cy5.5 is a CY dye. CY, short for Cyanine, is a compound consisting of two nitrogen atoms connected by an odd number of methyl units. Cyanine compounds have the characteristics of long wavelength, adjustable absorption and emission, high extinction coefficient, good water solubility and relatively simple synthesis. CY dyes are of en used for the labeling of proteins, antibodies and small molecular compounds. For the labeling of protein antibodies, the combination can be completed through a simple mixing reaction. Below, we introduce the labeling method of protein antibody labeling, which has certain reference significance.

Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.

Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

Nicotinamide riboside Chloride, an orally active NAD⁺ precursor, increases NAD⁺ levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.

Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i of 6.3 and 4.2 nM, respectively. [¹¹C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Folic acid (Vitamin B9) is a orally active essential nutrient from the B complex group of vitamins. Folic acid shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid can be used to the research of megaloblastic and macrocytic anemias due to folic deficiency.

Dimethyl 2-oxoglutarate (Dimethyl α-ketoglutarate) is a cell-permeable derivative of 2-oxoglutarate and tricarboxylic acid cycle metabolite with antioxidant properties. Dimethyl 2-oxoglutarate inhibits Autophagy. Dimethyl 2-oxoglutarate prevents mitochondrial damage and reduces ROS production. Dimethyl 2-oxoglutarate alleviates Carbon tetrachloride (HY-Y0298)-induced liver fibrosis. Dimethyl-2-oxoglutaric acid can be used in the research of diseases such as Alzheimer's disease, diabetes, and cardiomyopathy.

Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.

L-Carnitine ((R)-Carnitine), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine is an antioxidant. L-Carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism.