(D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity[1][2][3].
Deoxynyboquinone (NSC 165572;DNQ) is a potent inducer of cancer cell death that induces death of cancer cells in culture with IC50 of 16-210 nM, a substrate for NAD(P)H:quinone oxidoreductase (NQO1); it's lethality relies on NQO1-dependent futile redox cycling that consumes oxygen and generates extensive reactive oxygen species (ROS).
E(c(RGDfK))??is an αvβ3 integrin-specific binding moiety with tumor targeting properties. Increased uptake of E(c(RGDfK))??in human ovarian cancer OVCAR-3 xenograft tumors may be useful in cancer research[1].
SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.IC50 Value: 1.0 uM [1]Target: p38 MAPKin vitro: SB 242235 inhibited intracellular p38 activity, human chondrocytes were treated with different doses of SB 242235 prior to stimulation with IL-1_ for 15 min. MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. SB 242235 dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 uM [1].in vivo: SB-242235 demonstrates generally favourable pharmacokinetic properties in all species examined(including rat, dog and monkey). Systemic plasma clearance was high in rat, but in the non-rodent species SB-242235 demonstrated low to moderate clearance with plasma half-lives > 4h. Oral bioavailability in each preclinical species was high. In rat and monkey, SB-242235 demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses [2].In the skin of SKH-1 hairless mice, SB242235, prior to UVB irradiation, blocked activation of the p38 MAPK cascade, and abolished MAPKAPK-2 kinase activity and phosphorylation of HSP27. Moreover, SB242235 inhibited expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2 [3]. The preclinical pharmacokinetics of SB-242235 have been described previously. The present studies were conducted to describe the in vitro metabolic rates and routes of SB-242235 metabolism, to characterize its in vivo preclinical metabolism, and to use these data to aid in the prediction of the pharmacokinetic behaviour of SB-242235 in man [4].
(S)-ATPO is the (S)-enantiomer of ATPO, which is a competitive antagonist at GluR1-4 (AMPA-preferring) receptors[1].
3-Hydroxy-5,7,4′-trimethoxyflavone is a flavonol can be isolated from Cucubalus baccifer (L.)[1].
Clavulanate lithium is a potent β-lactamase inhibitor and acts as an antibiotic[1][2].
Dehydropachymic acid is one of the major triterpenes isolated from Poria cocos. Dehydropachymic acid is more effective in autophagy-lysosome pathway (ALP) impaired cells rather than normal cells[1].
Astraganoside, an isoflavane compound, isolated from the roots of Astragalus membranaceus (known as ‘‘Huangqi’’)[1].
NCRW0005-F05 is a potent GPR139 agonist with an IC50 value of 0.21 μM. NCRW0005-F05 can be used to research diabetes, obesity and Parkinson's disease[1].
Maculosin is a host-specific phytotoxin for spotted knapweed from Alternaria alternata. Maculosin is a quorum-sensing molecule involved in cell-cell communication by Pseudomonas aeruginosa. Maculosin also acts as a signaling molecule regulating virulence gene expression in Lactobacillus reuteri. Maculosin shows antioxidant, anti-cancer and non-toxicity properties. Maculosin shows cytotoxic activity against the human liver cancer cell lines, with an IC50 of 48.90 µg/mL[1][2][3].
Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. Ablukast effectively reduces LTC4- and antigen-induced bronchoconstriction[1][2]. Ablukast is LTD4 receptor antagonist[3].
Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM[1].
PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM); increases action potential rheobase in small diameter mDRG neurons, demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.
(Glu24)-Glucagon (1-29) (human, rat, porcine) is a fragment of glucagon.
(((9H-Fluoren-9-yl)methoxy)carbonyl)-D-lysine is a lysine derivative[1].
Condurango glycoside E0 is a glycoside that can be isolated from Marsdema cundurango[1].
HTBA(3-Hydroxy-2,4,6-triiodobenzoic acid) for your research needs.Off-white to yellow powder.
Echinocandin B (A 30912) is an antifungal antibiotic and is the secondary metabolite produced by Aspergillus nidulans[1].
NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.
Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways[1][2].
Raludotatug is a humanized immunoglobulin G1-kappa, anti-CDH6 monoclonal antibody. Raludotatug is an antineoplastic[1].
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively[1].
Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells[1].
Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway [1].
WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM[1][2]. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice[3].
Lumogallion is a highly sensitive fluorescent reagent for the detection of aluminum, gallium and other metals. Lumogallion has an excitation wavelength of 490 nm and an emission spectrum in the range of 520 nm to 650 nm, with a peak near 580 nm[1][2].
Glycolithocholic acid sodium is the sodium salt of Glycolithocholic acid. Glycolithocholic acid is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC)[1][2].
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride[1]. Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway[2].