Neurological Disease

NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor.

Acein is a novel nonapeptide, H-Pro-Pro-Thr-Thr-Thr-Lys-Phe-Ala-Ala-OH. Acein can promote the release of dopamine. Acein targets angiotensin converting enzyme (ACE I). Angiotensin converting enzyme (ACE I) can be used in nervous system related research.

ATM4 4-Acetoxy analog is an impurity in the synthesis of Heroin.

(Rac)-Tamsulosin (YM12617 (free base); (Rac)-LY253351 (free base)) is an isomer of Tamsulosin (HY-B0661). (Rac)-Tamsulosin is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α₁-adrenoceptors. (Rac)-Tamsulosin inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC₅₀ and K_i of 6.75 μM. (Rac)-Tamsulosin produces dose-dependent hypotension, preferentially antagonizing α₁-adrenoceptor-mediated pressor responses, and inhibits α₂-adrenoceptor-mediated pressor responses at high doses. (Rac)-Tamsulosin can be used in research related to various diseases such as metabolism.

Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC₅₀=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC₅₀=35 µM). Senktide TFA is promising for research of neurological disease.

AChE-IN-39 (Compound 7c) is an AChE inhibitor (IC₅₀: 0.058 μM). AChE-IN-39 has DPPH scavenging activity. AChE-IN-39 improves the cognitive impairment in AlCl₃-induced amnesia animal model. AChE-IN-39 can be used for research of Alzheimer's disease.

HDAC8-IN-15 is a selective HDAC8 inhibitor with an IC₅₀ of 0.40 μM. HDAC8-IN-15 increases the acetylation level of the HDAC8 substrate SMC3 without altering the total protein level of SMC3. HDAC8-IN-15 reduces cancer cell viability, inhibits colony formation, slows cell migration, induces apoptosis, and causes cell cycle arrest at the SubG1 phase. HDAC8-IN-15 can be used in studies related to neuroblastoma.

AVLX-144 is a highly potent inhibitor of postsynaptic density protein 95 (PSD-95). AVLX-144 can be used as a template to develop imaging probes for postsynaptic density (PSD) molecules, and can be labeled with fluorine-18 (¹⁸F) or tritium (³H) to visualize PSD-95 in vivo. AVLX-144 can be utilized for the study of Parkinson's disease.

α-Synuclein (67-78) (human) is the 67-78 fragment of α-Synuclein. α-Synuclein (67-78) (human) promotes network activity drive and blocks KCl-induced syt1L-ab uptake.

SGE-301 is a positive, allosteric NMDAR modulator. SGE-301 recovers NMDAR density and long-term potentiation to normal values. SGE-301 can be used in the research of neurological disorders.

Norisocorydine ((+)-Norisocorydine) is an aporphine alkaloid with antinociceptive and radical scavenging effects. Norisocorydine shows a SC₅₀ of 14.1 μg/mL in DPPH radical scavenging test. Norisocorydine exhibits antinociceptive ability in mice.

AChE activator 1 (compound 13) is a non-pyridinium oxime reactivator of paraoxon-inhibited acetylcholinesterase(AChE).

Lycopodiastrum casuarinoides extract (Lepidotis casuarinoides extract) is an extract of Lycopodiastrum casuarinoides that has acetylcholinesterase (AChE) inhibitory activity.

NYY-6a is a Ferroptosis inhibitor. NYY-6a shows significant inhibitory activity against RSL3-induced ferroptosis across 786-O and HT-1080 cells with EC₅₀s of 52 and 50 nM, respectively. NYY-6a functions as a radical trapping antioxidant (RTA) with efficacy of diminishing lipid peroxidation comparable to ferrostatin-1 and liproxtatin-1. NYY-6a is potential for ferroptosis related pathologies reasearch.

HYF038 is a blood-brain barrier-penetrant ligand of apoptosis signal-regulating kinase 1 (ASK1). When labeled with ¹¹C, HYF038 can be used for ASK1 neuroimaging studies.

Uperolein is a physalaemin-like endecapeptide, produced in the skin of Uperoleia rugosa and Uperoleia marmorata. Uperolein has a spasmodic effect on both the gastrointestinal tract and longitudinal muscles.

Schistoflrfamide, a FMRFamide-related peptide, is an inhibitory neuropeptide. Schistoflrfamide decreases the amplitude and frequency of myogenic contractions and reduce basal tension visceral muscle.

Eseramine is a weak acetylcholinesterase inhibitor with an IC₅₀ value of 9300 nM. Eseramine is promising for research of diseases involving the regulation of acetylcholinesterase, such as glaucoma, myasthenia gravis, and protection against organophosphate poisoning.

Articaine (Hoe-045) is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC₅₀ of 15.8 μM for open-state Na⁺ channels, and IC₅₀ of 40.6 μM and 378 μM for inactivated and resting-state Na⁺ channels, respectively. Articaine exerts local anesthetic activity by inhibiting Na⁺ influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury).

Agitoxin-2 TFA is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).