ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma[1][2][3].
1,2,3,4-Tetramethylbenzene consists of a benzene ring with four methyl groups (-CH3) as a substituent. 1,2,3,4-Tetramethylbenzene is a specialty product for biochemistry research[1].
PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. IC50 value: 0.37 nM [1]Target: PDE10APDE10A subcutaneously administrated at dose of 1 mg/kg elevates striatal cGMP about 3 fold in male CD-1 mice, while PDE10A subcutaneously administrated at dose of 3.2 mg/kg displays a maximal elevation of striatal cGMP approximately a 5-fold increase in male CD-1 mice. PDE10A intravenous injected at a dose of 0.1 mg/kg in Sprague-Dawley rats displays clearance of 36 ml/min/Kg, DE10A intravenous injected at a dose of 0.3 mg/kg in Dog Beagle displays clearance of 7.2 ml/min/Kg in vivo clearance with a moderate volume of distribution, DE10A intravenous injected at a dose of 0.03 mg/kg in Monkey Cynomolgus displays clearance of 13.9 ml/min/Kg in vivo clearance with a moderate volume of distribution. PDE10A is active with an ED50 of 1 mg/kg at a significantly lower total plasma exposure (115 nM) in the conditioned avoidance response assay (CAR) in Sprague-Dawley rats [1]. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity [2].
Z-Gly-Pro-AMC is a fluorogenic substrate. Z-Gly-Pro-AMC is hydrolyzed by prolyl endopeptidase to generate highly fluorescent 7-amido-4-methylcoumarin (HY-D0027). (λex=380 nm, λem=465 nm)[1].
Sodium gluconate is a corrosion and scale inhibitor of ordinary steel in simulated cooling water.
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM[1]. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2].
Luliconazole(NND 502) is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.IC50 Value: Target: AntifungalLuliconazole is an antifungal that belongs to the azole class. Although the exact mechanism of action against dermatophytes is unknown, luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase. Inhibition of this enzyme’s activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol. In a fertility study in rats, subcutaneous doses of 1, 5 and 25 mg/kg/day luliconazole were administered prior to and during mating and through early pregnancy. Treatment related effects on reproductive function were noted in females (decreased live embryos and decreased corpus luteum) at 5 and 25 mg/kg/day and males (decreased sperm counts) at 25 mg/kg/day. No treatment related effects on fertility or reproductive function were noted at 1 mg/kg/day (0.1X MRHD based on BSA comparisons).
BMS-582949 hydrochloride is a novel highly selective p38α MAPK inhibitor, inhibits p38α with IC50 of 13 nM. IC50 value: 13 nM[1]Target: p38αin vitro: BMS-582949 does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 with IC50values >40 μM. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. BMS-582949 is also 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective over Raf[1].BMS-582949 is a novel highly selective p38α MAPK inhibitor [2]. in vivo: The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And, at an oral dose of 10 mg/kg, the mouse AUC0?8 h for BMS-582949 is 75.5 μM·h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].
O-((Perfluorophenyl)methyl)hydroxylamine-d2 (hydrochloride) is the deuterium labeled O-((Perfluorophenyl)methyl)hydroxylamine hydrochloride[1].
SRTCX1003 is an orally active SIRT1 activator. SRTCX1003 suppresses inflammatory responses[1].
Vatiquinone is a potent cellular oxidative stress protectant, which could be used to treat mitochondrial diseases.
Rentiapril racemate is the racemate of Rentiapril. Rentiapril is an angiotensin converting enzyme (ACE) inhibitor.
Propargyl-PEG11-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Digoxigenin bisdigitoxoside is an anticancer drug. Digoxigenin bisdigitoxoside is cytotoxic[1].
2'-OMe-Ac-C Phosphoramidite is a modified phosphoramidite and can be used for the oligonucleotide synthesis.
Tetra-n-propyl-ammonium-d28 (bromide) is the deuterium labeled Tetra-n-propyl-ammonium bromide[1].
Ropinirole-d4 (SKF 101468-d4) hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[1][2].
Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity[1]. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells[2].
Cyclic di-GMP (c-di-GMP) diammonium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].
DMT-2′Fluoro-dU Phosphoramidite could be used for nucleoside modification.
Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.
NSC668394 (NSC 668394) is a small molecule inhibitor of ezrin, directly bind to ezrin with Kd of 12.59 uM; inhibits T567 phosphorylation and actin binding of endogenous ezrin at 10 μM without altering cellular ezrin levels, inhibits PKC-Ι phosphorylation of recombinant ezrin with IC50 of 8.1 uM; inhibits ezrin-mediated invasion of K7M2 OS cells, inhibits cell motility during zebrafish and Xenopus embryonic development; also inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung.
TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC50s of 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively[1].
ICG-alkyne is a click chemistry reagent containing an azide group[1].
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice[1].
Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC50 of 12 nM.
Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM[1][2].
PC Biotin-PEG3-NHS ester is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.