6-Aminocaproic acid-d10 (EACA-d10) is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
MLS1082 is a novel positive allosteric modulator of the D1 dopamine receptor, potentiatse dopamine-stimulated G-protein- and β-arrestin-mediated signaling and increase the affinity of dopamine for the D1 receptor with low micromolar potencies.
6-Hydroxyluteolin 7-glucoside is a flavonoid from Tanacetum parthenium and T. vulgare. 6-Hydroxyluteolin 7-glucoside inhibits the major pathways of arachidonate metabolism in leukocytes. 6-Hydroxyluteolin 7-glucoside has anti-inflammatory effect[1].
Genistein 8-c-glucoside (G8CG) is a natural glucoside isolated from flowers of Lupinus luteus L. Genistein 8-c-glucoside induces mitochondrial membrane depolarization and induces apoptosis[1].
Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder[1][2].
Amaronol A is an auronol, that can be isolated from the bark of Pseudolarix amabilis[1].
Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection[1][2].
5,6-trans-Vitamin D3 (5,6-trans-Cholecalciferol;5,6-trans-Colecalciferol) is a photoproduct of vitamin D3[1]. Vitamin D3 is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Naratriptan-d3 is the deuterium labeled Naratriptan[1]. Naratriptan is a selective 5-HT1 receptor subtype agonist[2].
Secretin, canine is an endocrine hormone that stimulates the secretion of bicarbonate-rich pancreatic fluids. Secretin, canine can regulates gastric chief cell function and paracellular permeability in canine gastric monolayers by a Src kinase-dependent pathway[1].
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM)[2].
6-methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
τ-Benzyl-Nα-(tert-butoxycarbonyl)-L-histidine is a histidine derivative[1].
Atuzaginstat (COR388) hydrochloride is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for Alzheimer's disease research[1][2].
Icaritin(Anhydroicaritin) is a component of Epimedium flavonoid isolated from Herba Epimedii; enhances osteoblastic differentiation of mesenchymal stem cells (MSCs) while it inhibits adipogenic differentiation of MSCs by inhibiting PPAR-g pathway.IC50 value:Target: in vitro: Icaritin was unable to promote proliferation, migration and tube like structure formation by human umbilical vein endothelial cells (HUVECs) in vitro [1]. Icaritin potently inhibited proliferation of K562 cells (IC50 was 8 μM) and primary CML cells (IC50 was 13.4 μM for CML-CP and 18 μM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis [2]. icaritin strongly inhibited the growth of breast cancer MDA-MB-453 and MCF7 cells. At concentrations of 2-3 μM, icaritin induced cell cycle arrest at the G(2)/M phase accompanied by a down-regulation of the expression levels of the G(2)/M regulatory proteins such as cyclinB, cdc2 and cdc25C. Icaritin at concentrations of 4-5 μM, however, induced apoptotic cell death characterized by the accumulation of the annexin V- and propidium iodide-positive cells, cleavage of poly ADP-ribose polymerase (PARP) and down-regulation of the Bcl-2 expression [3].in vivo: In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or time-dependent manner [2].
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity[1].
Ovothiol C (Medkoo;Ovothiol C) is a natural product that can be found in eggs or ovarian tissue[1].
DMT-dC(ac) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
2′-Deoxy-2′-fluoroadenosine can be used for the synthesis of 2′-Deoxy-2′-fluoro-modified oligonucleotides hybridized with RNA. 2′-Deoxy-2′-fluoroadenosine can be cleaved efficiently by E. coli purine nucleoside phosphorylase (PNP) to the toxic agent 2-fluoroadenine (FAde) and shows excellent in vivo activity against tumors expressing E. coli PNP[1].
3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) is a potent dopamine uptake inhibitor[1]. 3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) acts as a potent long-acting antihistaminic agent[2].
N-(3,5-Dinitrobenzoyl)-DL-leucine is a leucine derivative[1].
DL-Carnitine is a racemic mixture of L-Carnitine and D-Carnitine, regulates fatty acid transport in mitochondria, elevates serum carnitine fractions.
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
3’-β-C-Ethynyluridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
Chitobiose dihydrochloride, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units[1].
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors[1].
C18(plasm)-18:1 PC-d9 is deuterium labeled C18(plasm)-18:1 PC.
NH2-KAA-COOH is a oligopeptide compoused of Lys-Ala-Ala.
RFRP-1(human) is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
N4,N4-Dimethylarabinocytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].