Neurological Disease

(E/Z)-Piperine ((E/Z)-Bioperine) is an alkaloid with a pungent property. (E/Z)-Piperine shows anti-inflammation, immunomodulatory and anti-cancer, antispasmodic and anti-secretory effects. (E/Z)-Piperine demonstrates significant neuroprotective effect in Alzheimer’s disease and Parkinson’s disease.

Iprindole hydrochloride, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole hydrochloride shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole hydrochloride induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression.

CAII/VII-IN-1 is an orally active hCA II (K_I = 12.3 nM), and hCA VII (K_I = 22.6 nM) inhibitor, showing no significant activity against hCA I. CAII/VII-IN-1 shows excellent neuroprotective activity in vivo Pilocarpine (HY-B0726A)-induced seizure model. CAII/VII-IN-1 can upregulate KCC2 and inhibit mTOR, exerting neuroprotective effects. CAII/VII-IN-1 does not show any significant neurotoxic effects or alterations in liver and kidney function. CAII/VII-IN-1 can be used for the study of epilepsy.

Secretin (33-59), rat is a 27-aa peptide, acts on secretin receptor, enhances the secretion of bicarbonate, enzymes, and K⁺ from the pancreas.

Orexin B, human-¹³C₆,¹⁵N (Human orexin B-¹³C₆,¹⁵N) TFA is the ¹³C- and ¹⁵N-labeled Orexin B, human (HY-P1339). Orexin B, human is the agonist for Orexin Receptor, with K_is of 420 nM and 36 nM for OX1 and OX2. Orexin B, human participates in the regulation of appetite, wakefulness, cardiovascular function and neuroendocrine.

6-Methoxykaempferol 3-O-Rutinoside is a natural product isolated from the herbs of Pilocarpus pennatifolius.

Hexanoylglycine-¹³C₂,¹⁵N is the ¹³C- and ¹⁵N-labeled Hexanoylglycine (HY-113150). Hexanoylglycine is an endogenous metabolite present in Urine that can be used for the research of Ethylmalonic Encephalopathy.

OX₂R-IN-1 (compound 15) is a low cytotoxicity profile OX₂R-IN-1 antagonist (a potential OX2R binder) with an IC₅₀ value of 484 μM. OX₂R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life.

Ledasorexton is an orally active OX2R agonist (EC₅₀: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease.

EVP-21 is a selective TRPML3 agonist with an EC₅₀ of 4.3 μM for human TRPML3. EVP-21 elicits TRPML3 currents in late endosomes/lysosomes and early endosomes. EVP-21 can be used for research on TRPML3-related mechanisms such as emphysema, hearing loss, and yellow fever virus infection.

E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (K_i=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.

Norharmane (Standard) is the analytical standard of Norharmane. This product is intended for research and analytical applications. Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings.

Elzasonan citrate (CP-448187 citrate) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.

HJ03 is a blood-brain barrier-permeable, orally active DNA damage and ferroptosis inducer. HJ03 triggers ferroptosis by increasing intracellular ROS, Fe²⁺ accumulation and lipid peroxidation. HJ03 induces DNA adducts and interstrand crosslinks, blocks DNA replication and transcription, arrests cells at the G2/M phase and induces apoptosis. HJ03 can be used in the research of glioblastoma multiforme and colorectal cancer.

D156844 (Compound 11a) hydrochloride is a SMN2 promoter activator with an EC₅₀ of 4 nM. D156844 hydrochloride increases the mRNA expression of the mouse SMN in NSC-34 cells and human SMN2 promoter in severe type I spinal muscular atrophy (SMA) fibroblasts as well as full-length human SMN protein. D156844 hydrochloride overcomes DHFR inhibition. D156844 hydrochloride can be used for SMA research.

PF-1010 is a CD73 inhibitor with an IC₅₀ ranging from 101 to 1000 nM. PF-1010 blocks the interaction between CD73 protein and its substrate, and inhibits the enzymatic activity of CD73. PF-1010 is applicable to the research of cancer, infectious diseases, autoimmune diseases and neurodegenerative diseases.

N-Desmethyl imatinib-d₄ is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

Bupivacaine hydrochloride solution is mainly composed of Bupivacaine hydrochloride monohydrate (HY-W415121). Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.

β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.

SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC₅₀s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with K_is of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research.