Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). IC50 value:Target: DPP4Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.
ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
Homoeriodictyol 7-O-β-D-glucoside is a natural platelet-activating factor (PAF) antagonist. Homoeriodictyol 7-O-β-D-glucoside inhibits human and rabbit platelet aggregation induced by PAF, with an IC50 of 0.8 μM[1].
Paucimannose is a common mannosidic N-glycoepitope that exists in invertebrates and plants. paucimannosidic glycans are expressed in cancers[1].
Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein vitro: Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase [1]. in vivo: Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone [2]. Febuxostat prevents hyperuricemia in 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups [3]. Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC) attenuates the TAC-induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC-induced increases in nitrotyrosine (indicating reduced myocardial oxidative stress), p-Erk(Thr202/Tyr204), and p-mTOR(Ser2488), with no effect on total Erk or total mTOR [4].
Ethyl 2-bromopropionate-d3 is the deuterium labeled Ethyl 2-bromopropionate[1].
7-Propargyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
E-982 is extracted from the reference, compound 12.
CEF1, Influenza Matrix Protein M1 (58-66) is an epitope derived from the matrix protein of the influenza A virus[1].
DNMT3A-IN-2 (compound 2) is a potent and allosteric inhibitor of DNMT3A. DNMT3A-IN-2 inhibits DNMT3A activity by disrupting protein-protein interactions. DNMT3A-IN-2 induces apoptosis of acute myeloid leukemia (AML) cell lines. DNMT3A-IN-2 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].
Boc-NH-PEG7-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
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].
YMRF-NH2 is a neuropeptide. YMRF-NH2 binds to FMRFa-R with an EC50 value of 31 nM[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].
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo[1][2].
KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
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].
Gentiournoside D is a natural compound that can be found in G. asclepiadea extracts[1].
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.
Fmoc-DON-Boc (Compound 8b) is an Fmoc-protected compound that can be used for the synthesis of proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357). DON is a glutamine antagonist[1].
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]