GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity[1][2].
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
N-(Azido-PEG2)-N-Boc-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Bis-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
16:0-18:1 PG-d31 is deuterium labeled 16:0-18:1 PG.
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA) with the MIC90 value of 2 mcg/mL.
RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
TES sodium is a buffering agent (pKa=7.550 at 25°C). TES sodium is one of the Good's buffers, the buffer capacity ranging pH 6.8-8.2[1][2].
MCI826 is a P-glycoprotein (P-gp) antagonist.
TH-237A(meso-GS 164) is a novel neuroprotective agent exhibiting favorable permeation across the blood brain barrier.IC50 value: 5 nM (EC50, concentration that leads to a 50% increase in neuronal survival in the presence of the Aβ peptides)Target: Primary neurons were isolated from embryonic Sprague-Dawley rats, grown in culture (Michaelis et al., 1994) and exposed to either Aβ25-35 or Aβ1-42 in the presence or absence of TH-237A at concentrations ranging from 0.5 to 60 nM. The neurons were treated with TH-237A for 2 hours prior to exposure to the Aβ peptides. Changes in neuronal survival following treatment with TH 237A were evaluated using the Live/Dead assay. The EC50 for TH-237A was 5 nM, demonstrating that it had excellent neuroprotective properties.
ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor[1]. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease[2].
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitory activity against cyclooxygenase-1, with the IC50 value of 30.4 μM[1].
N-(Azido-PEG3)-N-Boc-PEG4-acid is a PEG-based PROTAC linker with a terminal azide group and is used in the synthesis of PROTACs[1]
Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.Target: Dopamine ReceptorChlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with Ki values of 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (Ki >1000 nM) [1]. Chlorprothixene also shows high affinities for both rat 5-HT6 from stably transfected HEK-293 cells, and rat 5-HT7 receptors from transiently expressed COS-7 cells, with Ki values of 3 nM and 5.6 nM, respectively [2].Administration of Chlorprothixene restores normal ceramide concentrations in murine bronchial epithelial cells, reduces inflammation in the lungs of mice with cystic fibrosis (CF) and prevents infection with Pseudomonas aeruginosa, by inhibiting acidsphingomyelinase (Asm) and not neutral sphingomyelinase (Nsm) [3].
Flurbiprofen axetil is a non-selective cyclooxygenase (COX) inhibitor. Flurbiprofen axetil has anti-inflammatory effect[1].
Carisbamate (RWJ-333369) is an orally active neuromodulator. Carisbamate prevents the development and production of epilep-like discharges and has a neuroprotective effect after in vitro epilepticus-like injury. Carisbamate has good antiepileptic activity in genetic models of generalized and nonconvulsive epilepsy[1][2][3].
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Rotigotine Hydrochloride is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
FASN-IN-1 is a fatty acid synthase (FASN) inhibitor extracted from patent WO2015134790A1, compound 56[1].
Sunset Yellow FCF is a petroleum-derived orange azo dye with a pH dependent maximum absorption at about 480 nm at pH 1 and 443 nm at pH 13. Sunset Yellow is used in food, cosmetics, and drugs.
Moroxydine HCl is a synthetic antiviral compound chemically belonging to the series of the heterocyclic biguanidines.Target: Influenza VirusMoroxydine is an antiviral drug that was originally developed in the 1950s as an influenza treatment. It has potential applications against a number of RNA and DNA viruses [1]. Structurally moroxydine is a heterocyclic biguanidine. Moroxydine was reported in March 2014 that three kindergartens in two provinces of China had been found to be secretly dosing their students with moroxydine hydrochloride to try to prevent them from becoming ill. The kindergartens are paid only for the days that pupils attend and wanted to ensure that they maximised their earnings [2].
4-Aminobenzonitrile-d4 is the deuterium labeled 4-Aminobenzonitrile[1].
Hibiscetin heptamethyl ether is a natural product isolated from various medicinal plants[1].
ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro[1][2].
Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.
DSPE-SPDP is a phospholipid molecule. DSPE-SPDP can orient itself to form lipid bilayer in water. DSPE-SPDP can be used for the research of various biochemical[1].
Seletracetam (Ucb 44212) lithium bromide, an analog of the antiepileptic agent Levetiracetam, is a SV2A modulator for the research of epilepsy[1][2][3].
Tianagliflozin is a sodium/glucose cotransporter 2 (SGLT-2) inhibitor with potential for investigation in type 2 diabetes[1].