AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain.
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.IC50 value: 7.6/14/3.7 nM(mouse/rat/human MAGL) [1]Target: MAGL inhibitorJW 642 is selective for MAGL, requiring much higher concentrations to effectively inhibit fatty acid amide hydrolase activity (IC50s = 31, 14, and 20.6 μM for mouse, rat, and human brain membranes, respectively).
S-Methyl-L-cysteine is a natural product that acts as a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductase A (MSRA), with antioxidative, neuroprotective, and anti-obesity activities.
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways[1]. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons[2].
BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation[1].
(S)-MCPG is the active isomer of (RS)-MCPG (Cat. No. HY-100371), non-selective group I/group II metabotropic glutamate receptor antagonist. In vivo: (S)-MCPG (20.8 μg) injected intraventricularly (i.c.v.) before testing impaired the performance of rats in the spatial version of the Morris water maze, but 1/10 of this dose did not. Memory retention, evaluated 24 hr post-training, is also affected by the high dose of MCPG.
Kinetin (N6-furfuryladenine) belongs to a group of plant growth hormones involved in cell division, differentiation and other physiological processes.IC50 Value: Target:Kinetin is one of the widely used components in numerous skin care cosmetics and cosmeceuticals, such as Valeant products kinerase. Recently, kinetin has the potential to be a treatment for the human splicing disease familial dysautonomia.in vitro: Kinetin-induced cell death reflected by the morphological changes of nuclei including their invagination, volume increase, chromatin condensation and degradation as well as formation of micronuclei showed by AO/EB and 4,6-diamidino-2-phenylindol staining was accompanied by changes including increase in conductivity of cell electrolytes secreted to culture media, decrease in the number of the G1- and G2-phase cells and appearance of fraction of hypoploid cells as the effect of DNA degradation without ladder formation [1]. The plant cytokinin kinetin dramatically increases exon 20 inclusion in RNA isolated from cultured FD cells [3].in vivo: Subjects received 23.5 mg/Kg/d for 28 d. An increase in WT IKBKAP mRNA expression in leukocytes was noted after 8 d in six of eight individuals; after 28 d, the mean increase compared with baseline was significant (p = 0.002) [2].Toxicity: On mice with leukaemia P388, kinetin has no effect on the tumour growth, and it appears to be toxic at the dose of 25 mg/kg [4].
Carabersat is a potent anticonvulsant agent.
MRS2698 is a potent and highly selective P2Y2 receptor agonist with an EC50 of 8 nM. MRS2698 is >300-fold P2Y2-selective versus the P2Y4 and P2Y6 receptors[1][2].
Piribedil is a dopamine D2 receptor (D2R) agonist which also displays antagonist property at hα1A-adrenoceptor (hα1A-AR).
Tyr-Somatostatin-28 is a somatostatin that adds a Tyrosine amino acid to Somatostatin-28[1].
Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease[1].
threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity[1][2][3].
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].
ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC50 value of 20 μM.
1-Benzyl-1,2,3,4-tetrahydro-isoquinoline is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Parkinson's Disease[1][2].
Angeloylgomisin Q is a new dibenzocyclooctadiene lignan from the stems of Schisandra sphaerandra[1]. Angeloylgomisin Q has the potential for alzheimer's disease research[2].
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM)[1].
(Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist[1].
ALX-5407 ((R)-NFPS) hydrochloride is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 hydrochloride can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia[1].
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[1]. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation[2].
Memantine-d6 hydrochloride is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
NCC-149 is a selective HDAC8 inhibitor and can be used for neural differentiation research[1].
TP-030-2 is a RIPK1 inhibitor (human Ki=0.43 nM; mouse IC50=100 nM)[1][2].
Ozanimod (hydrochloride) (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod (hydrochloride) (RPC-1063) has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod (hydrochloride) (RPC-1063) can be used for the research of relapsing multiple sclerosis (MS) [1].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively[1].
VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM[1].