Neurological Disease

DR-4004 is a 5-HT₇ receptor antagonist that attenuates the decreased level of performance produced by mCPP and the performance levels after p-chloroamphetamine (PCA) lesion of the 5-HT system. DR-4004 also reverses amnesia induced by Scopolamine (HY-N0296) and Dizocilpine (HY-15084B). DR-4004 is promising for research of schizophrenia, cognitive deficits and atypical antipsychotic agents.

8-Aminoclonazolam is a benzodiazepine and clonazolam metabolite.

N-Desmethyl Rilmazolam is a metabolite of Rilmazolam (HY-150334) and 450191-S (HY-U00228). N-Desmethyl Rilmazolam significantly enhances the activity of 7-ethoxycoumarin O-deethylase. N-Desmethyl Rilmazolam can be used in insomnia-related studies.

Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.

Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with K_i values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.

[His7] Corazonin, a neurohormone, induces dark color in the cuticle and epidermis of Locusta migratoria.

Cariprazine N-oxide (Compound DP-3) is the mono-oxidative degradation product of Cariprazine hydrochloride (HY-14763A). Cariprazine hydrochloride exhibits antipsychotic activity.

Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pK_i of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models.

EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC₅₀=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis.

Santacruzamate A (Standard) is the analytical standard of Santacruzamate A. This product is intended for research and analytical applications. Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research[1][2].

Biocytin (Standard) is the analytical standard of Biocytin. This product is intended for research and analytical applications. Biocytin is a conjugate of D-biotin and L-lysine, where the carboxylate of D-biotin is coupled with the -amine of L-lysine via a secondary amide bond. Biocytin is a classical neuroanatomical tracer commonly used to map brain connectivity. Biocytin is used as a versatile marker in anterograde, retrograde and intracellular neuroanatomical investigations and in biotinidase assays[1][2].

AChE-IN-94 is an orally active and blood-brain barrier penetrable AChE inhibitor with an IC₅₀ of 0.40 μM and K_i of 0.28 μM. AChE-IN-94 prevents self-induced and AChE-mediated Aβ_1-42 aggregation. AChE-IN-94 alleviates cognitive/memory deficits in Scopolamine (HY-N0296)-induced amnesic model. AChE-IN-94 can be used for the study of Alzheimer's disease (AD).

FAM labled Rovanersen sodiumis a FAM labled Rovanersen sodium.

Ganoleucoin R is a triterpenoid compound that can be isolated from Ganoderma leucocontextum. Ganoleucoin R exerts a protective effect against H₂O₂-induced oxidative damage and can promote neurite outgrowth in PC12 cells. Ganoleucoin R possesses neuroprotective and neurogenic activities, and can be used in the research of neurodegenerative diseases.

Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.

Nefopam-d₄ (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.

(R)-Dabelotine is the R-isomer of Dabelotine and functions as an adrenergic agonist, making it valuable in dementia research.

Aβ-IN-4 (compound 12) is a potent amyloid β (Aβ) inhibitor. Aβ-IN-4 inhibits Aβ42 aggregation. However, Aβ-IN-4 can not alleviate the neurotoxicity of Aβ42 in SH-SY5Y cells. Aβ-IN-4 can not change the aggregation state of Aβ42 into a nontoxic one.

Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model.