Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM[1].
1-Hexanol-d11 is the deuterium labeled 1-Hexanol[1]. 1-Hexanol, a primary alcohol, is a surfactant that can be employed in industrial processes to enhance interfacial properties[2]. 1-Hexanol uncouples mitochondrial respiration by a non-protonophoric mechanism[3].
Kuguacin R is a cucurbitane-type triterpenoid that can be extracted from Momordica charantia L. Kuguacin R possess anti-inflammatory, antimicrobial and anti-viral activities[1].
3-Nitrobenzoic acid-d4 is the deuterium labeled 3-Nitrobenzoic acid[1].
Decyl β-D-maltopyranoside is a biochemical reagent[1].
H-Phe(3,5-DiF)-OH is a difluorophenylalanines in the L-configuration [L-(F2)Phe]. H-Phe(3,5-DiF)-OH can be incorporated into the thrombin receptor-tethered ligand peptide SFLLRNP to identify the phenyl hydrogens of the Phe-2 residue involved in the CH/π receptor interaction[1].
Tiapride, an atypical neuroleptic agent, is a selective dopamine D2-receptor antagonist with little propensity for causing catalepsy and sedation. The IC50 values of Tiapride are 1440, 45.8, >100, and 11.7 μM for D1; D2; D3; D4, respectively[1].
(Trp4)-Kemptide is a peptide substrate for adenosine 3',5'-cyclic monophosphate-dependent protein kinase[1].
AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.IC50 value: 9.3 nMTarget: c-Metin vitro: AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM [1]. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation [2]. AMG-208 is identified to be a c-MET and RON dual selective inhibitor [3].in vivo: In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour[1].
Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo[1]. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia[2].
ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type β-catenin), respectively; remain affinity for muant catenin V511S, V511S/I569S and R469A with Ki of 20-50 uM; exhibits dual selectivity for β-catenin/Tcf over β-catenin/cadherin and β-catenin/APC PPIs.
Hexa-D-arginine is an inhibitor of furin.
Hydroxyevodiamine (Rhetsinine) inhibits aldose reductase with an IC50 value of 24.1 μM[1].
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis[1].
Oxytocin antiparallel dimer is the disulfide-bridged homo peptide dimer[1].
AZD1981 is a potent and selective CRTh2 antagonist; displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).IC50 value:Target: GPR44 antagonistin vitro: AZD1981 produced a concentration-dependent displacement of the [3H]PGD2-specific binding with a mean pIC50 of 8.4 ± 0.1 (n = 25, geometric mean IC50 of 4 nM). AZD1981 had no significant affinity towards recombinant human DP1 receptors with only a mean 27% (range 14–50%; n = 4) displacement of [3H]PGD2-specific binding observed at the highest concentration tested (10 μM). Compared with the binding potency for DP2, AZD1981 showed 10-fold selectivity over rat aldose reductase and 1700-fold selectivity over rat steroid 5α-reductase.In eosinophils, a single concentration of 1 μM, AZD1981 caused a large (20-fold) rightward parallel shift in the 15R-methyl PGD2 E/[A] curve with no evidence of a decrease in the maximal response. The effect of AZD1981 was therefore investigated using a single sub-maximal concentration of agonist (1 μM). AZD1981 produced a concentration-dependent inhibition of eosinophil migration with a pIC50 value of 7.6 ± 0.1 (n = 4) [1].in vivo: Using the previously described guinea pig hind limb model , 10 nM AZD1981 significantly inhibited DK-PGD2-induced eosinophil mobilization by approximately 50%, and the response was completely inhibited with 100 nM AZD1981 [1]. in vivo: AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow [1]. There was no beneficial clinical effect of AZD1981, at a dose of 1000 mg twice daily for 4 weeks, in patients with moderate to severe COPD. AZD1981 was well tolerated and no safety concerns were identified [3].
Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively[1][2][3][4][5].
Robalzotan hydrochloride (NAD-299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system[1][2][3].
Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
Oxybenzone(Eusolex 4360; Escalol 567) is an organic compound used in sunscreens; provides broad-spectrum ultraviolet coverage, including UVB and short-wave UVA rays.
Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis[1][2].
Clopamide is an orally active thiazide-like diuretic agent that inhibits the sodium-coupled chloride cotransporter SLC12A3. Clopamide has the potential for hypertension and cardiac failure research[1][2].
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC)[1].
Boc-D-Phe(2-Me)-OH is a phenylalanine derivative[1].
A potent, selective intermediate-conductance KCa3.1 positive-gating modulator with EC50 of 111 nM; displays 123-fold selectivity over KCa2.3 (EC50=13.7 uM), and 200- to 400-fold selective over representative KV, NaV, as well as CaV1.2 channels; not only lowers blood pressure but also drastically reduces heart rate, presumably through cardiac and neuronal KCa2 activation in mice.
7-Methyl-diguanosine triphosphate (m7Gp3G) is a cap analog that can incorporated into mRNA. 7-Methyl-diguanosine triphosphate is involved in translation and mRNA degradation in mammalian cells[1].
Alcesefoliside is a flavonoid isolated from Nitraria sibirica Pall, with antioxidant activity[1].
Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.