Neurological Disease

HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with K_is of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.

AChE/PDE4-IN-1 (compound 12c) is a potent and selective dual PDE4/AChE inhibitor, with IC₅₀s of 0.28 μM and 1.88 μM for AChE and PDE4D, respectively. AChE/PDE4-IN-1 exhibits anti-neuroinflammatory effect for the research of Alzheimer's disease.

RO 16-6491 Free base is a selective, reversible inhibitor of monoamine oxidase type B (MAO-B), exhibiting high affinity and specificity for binding sites in human frontal cortex mitochondria and platelet membranes. RO 16-6491 demonstrates a fast dissociation of bound radioactivity at 20 degrees C, indicating its dynamic binding properties. RO 16-6491 also acts as a substrate for MAO-B, suggesting that its oxidation may produce a stable intermediate responsible for its potent inhibitory effects. RO 16-6491 serves as an excellent radioligand probe for investigating the regional tissue distribution of MAO-B in various physiological and pathological states.

Sibiricose A5 (Standard) is the analytical standard of Sibiricose A5. This product is intended for research and analytical applications. Sibiricose A5 is an oligosaccharide ester isolated from Polygalae Radix with potent antioxidant activity.

4-(Acetoxymethyl)phenyl glucoside is a type of gastrodin derivative that can cross the blood-brain barrier. 4-(Acetoxymethyl)phenyl glucoside exhibits sedative, anticonvulsant and analgesic effects in mouse models. 4-(Acetoxymethyl)phenyl glucoside can be used for research on senile cardiovascular and cerebrovascular diseases as well as brain nerve disorders.

4-Guanidinobutanoic acid (Standard) is the analytical standard of 4-Guanidinobutanoic acid (HY-113286). This product is intended for research and analytical applications. 4-Guanidinobutanoic acid is a metabolite of arginine and an orally active SLC36A1/Hedgehog signaling pathway activator. 4-Guanidinobutanoic acid drives epithelial reprogramming, enhances intestinal stem cell function and goblet cell differentiation. 4-Guanidinobutanoic acid promotes the enrichment of Akkermansia muciniphila via mucus-dependent niche expansion, regulates intestinal homeostasis, and establishes a microbiota-host feedback loop. 4-Guanidinobutanoic acid exhibits anti-aging and healthspan-regulating properties. 4-Guanidinobutanoic acid can be used in research related to ulcerative colitis, amyotrophic lateral sclerosis, and Duchenne muscular dystrophy.

Parpanil is an anticholinergic agent with NMDA receptor antagonist activity. Parpanil can be used to inhibit diseases related to cholinergic neurotransmission. Parpanil exerts its pharmacological effects by blocking cholinergic effects.

(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability.

MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease.

DRP1 Allosteric-IN-1 (Compound 1) is an allosteric inhibitor of DRP1 with an IC₅₀ value for the DRP1:MiD49 protein-protein interaction of 3.6 μM. DRP1 Allosteric-IN-1 can be used to study various diseases related to mitochondrial division disorders.

(-)-Anatoxin A is an enantiomer of (±)-Anatoxin A (HY-N2326). (-)-Anatoxin A is a neuronal nicotinic acetylcholine receptor agonist. (-)-Anatoxin A can be used for pain and inflammation research.

Sarcandra glabra extract is an extract of Sarcandra glabra that can be used to improve mental efficiency and relieve stress or fatigue.

α-Synuclein (34-45) (human) is the 34-45 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly abundant in presynaptic nerve terminals. α-Synuclein is a Parkinson's disease (PD) biomarker.

mGluR7-IN-1 (compound 2Z) is a mGluR3 inhibitor.

Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC₅₀ of 14 nM; Valorphin also shows anti-tumor activity.

BMS-442606, the S-enantiomer of 6-hydroxybuspirone (6OHB), is an orally active 5-HT_1A partial agonist. BMS-442606 can be used for generalized anxiety disorder (GAD) research.

Metaxalone-d₆ is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABA_A receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.

Loreclezole hydrochloride, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

NS4591 is a modulator of calcium-activated potassium channels with activity that enhances small (SK) and intermediate (IK) conductivity. NS4591 doubled IK-mediated currents in whole-cell patch-clamp experiments at a concentration of 45 +/- 6 nM, and doubled SK3-mediated currents at a concentration of 530 +/- 100 nM. NS4591 inhibits the number of action potentials generated by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons. NS4591 also reduced carbakol-induced detrusor ring contraction in the rat bladder, demonstrating sensitivity to apamin.