Neurological Disease

Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging.

Kissoone C (compound 3) is a three-membered ring sesquiterpene isolated from valerian root. Kissoone C can enhance the activity of nerve growth factor (NGF)-mediated neurite outgrowth in PC12D cells.

Lurasidone-d₈-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

Fezolamine is an orally active non-tricyclic compound , and shows antidepressant activity.

(1R,2R)-Elpipodect ((1R,2R)-MK-8189) is the (1R,2R) enantiomer of Elpipodect (HY-153093). Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a K_i of 29 pM. Elpipodect can be used in research of schizophrenia.

Cinchona ledgeriana extract, derived from the cinchona tree, is rich in alkaloids such as quinine and quinidine, and has antimalarial, anti-inflammatory, analgesic, and antioxidant effects.

PIP5K1B participates in the biosynthesis of PI(4,5)P2. PIP5K1B is at the crossroad of different signaling pathways, mediating RAC1-dependent reorganization of actin filaments and contributing to the activation of phospholipase D2. PIP5K1B Recombinant Human Active Lipid Kinase can be used for the study of Friedreich’s ataxia (FRDA).

Sigma ligand-1 hydrochloride is a selective sigma receptor ligand with an IC₅₀s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 hydrochloride has a K_i of 4000 nM at the dopamine D₂ receptor.

TrkB agonist-1 is an orally active, blood-brain barrier-permeable TrkB agonist. TrkB agonist-1 activates the TrkB signaling pathway and its downstream AKT and ERK/MAPK pathways via its released parent compound, reduces AEP enzyme activity and inhibits its activation, and simultaneously suppresses the production of pro-inflammatory cytokines. TrkB agonist-1 is used in the research of Alzheimer's disease.

Quinagolide (CV205-502) is a non-ergot dopamine D(2) receptor agonist that promotes dopamine activity. Quinagolide has shown effectiveness in modulating endocrine function, particularly in inhibiting disorders associated with dopamine deficiency. Quinagolide is used to suppress hyperprolactinemia and corresponding clinical symptoms, showing good efficacy. Quinagolide's biological activity enables its use as an important research compound in drug isolation and analysis.

Perospirone-d₈ (SM-9018-d₈ (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT_2A receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.

NS163 is a α-Synuclein aggregation antagonist. NS163 can be used for study of Parkinson’s disease.

γ-Secretase modulator 11 (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.

SU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC₅₀ values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma.

RBI-257 maleate is a potent dopamine D4 receptor antagonist with a K_i value of 0.3 nM.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC₅₀s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonic anhydrase are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC₅₀s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain.

Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC₅₀ of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC₅₀s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research.

Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia.

TAU-IN-6 (Compound 13) is a Tau protein misfolding and aggregation inhibitor. TAU-IN-6 inhibits stress granules composed of tau and TIA1. TAU-IN-6 is applicable for Alzheimer's disease research.