Neurological Disease

Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a K_i of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.

ATX inhibitor 27 (Compound 31) is an ATX inhibitor. The IC₅₀ values of ATX inhibitor 27 against human autotaxin (hATX) and lysophosphatidylcholine (LPC) are 13 nM and 23 nM, respectively. ATX inhibitor 27 reduces LPA levels in vivo by inhibiting ATX enzyme. ATX inhibitor 27 can be used in the study of ATX-LPA-related diseases such as inflammation, neurodegenerative diseases and cancer.

S-14671 is a high-affinity 5-HT_1A agonist (pK_i=9.3). S-14671 can be used for research on neurological diseases, such as anti-anxiety, anti-depression, etc.

Piracetam-d₆ is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.

iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC₅₀ of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable.

Norcisapride is a metabolite of cisapride (HY-14149). Norcisapride can be converted into UNK under CYP3A4.

5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC₅₀s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.

FAM labled Tadnersen sodiumis a FAM labled Tadnersen sodium.

HDAC degrader-2 is a HDAC degrader, and its DC₅₀ for HDAC1 in MM.1S cells is 2.55 μM. HDAC degrader-2 recruits and covalently binds to DDB1, thereby inducing proteasomal degradation of HDAC1 and HDAC2. HDAC degrader-2 inhibits HDAC6 activity and increases the acetylation levels of α-tubulin and histone H3. HDAC degrader-2 induces early and late apoptosis and reduces the proliferative capacity of cancer cells. HDAC degrader-2 can be used for research on multiple myeloma and breast cancer.

TAN 950A is antifungal amino acid antibiotic. TAN 950A has affinity for three excitatory amino acid (EAA) receptor and can inhibit [3H]AMPA, [3H]kainite and [3H]CPP binding competitively. TAN 950A can be used for the researches of infection and neurological disease.

U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (K_i=0.2 nM).

ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC₅₀= 0.067 μM, TREK-2 IC₅₀= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.

[U-¹⁵N]-Aβ(1-40)/[U-¹⁵N]-Aβ(1-42) is the ¹⁵N-labeled Aβ(1-40) and Aβ(1-42). Abnormal levels and aggregation of beta-amyloid (Aβ) in the brain are considered key factors in the pathogenesis of Alzheimer's disease (AD). This isotope can be used in NMR studies of disease mechanisms and in mass spectrometry analysis.

Olprinone (Loprinone) hydrochloride hydrate is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC₅₀ values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone hydrochloride hydrate exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone hydrochloride hydrate can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury.

THIP-d₄ (Gaboxadol-d₄) is the deuterated-labeled THIP (HY-10232). THIP (Gaboxadol) is a blood-brain barrier-penetrant, orally active selective GABA_A receptor agonist. THIP exhibits EC₅₀ values of 33 μM and 130 μM for α₄β₂δ and α₄β₁δ receptors, respectively. THIP activates extrasynaptic GABA_A receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP is used in research on insomnia, sleep disorders, and addictive behaviors.

Dynorphin A (1-13) amide is an endogenous opioid peptide that antagonizes morphine-induced analgesia.

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ³⁵S binding to CHO_hNOP membranes with pK_i values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.

Thymidine phosphorylase is a nucleoside metabolism enzyme that plays an important role in the pyrimidine salvage pathway. Thymidine phosphorylase catalyzes the conversion of thymidine to thymine and 2-deoxy-α-D-ribose-1-phosphate (dRib-1-P). Thymidine phosphorylase plays an important role in platelet activation in vitro and thrombosis in vivo by participating in multiple signaling pathways. Thymidine phosphorylase can be used for the study of myocardial infarction, stroke, pulmonary embolism and cancer.

Isradipine-d₆ is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research.