LY3104607 is a potent, selective and orally available G Protein-Coupled Receptor 40 (GPR40) agonist with potential antidiabetic application. It has optimized pharmacokinetic properties to support once daily oral treatment in patients with Type 2 Diabetes Mellitus. LY3104607 demonstrated functional potency and glucose-dependent insulin secretion (GDIS) in primary islets from rats. Potent, efficacious, and durable dose-dependent […]

SHIP2-IN-1 is a novel and potent SHIP2 inhibitor which inhibits SHIP2 activity with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease. SH2 domain-containing inositol 5′-phosphatase 2 (SHIP2) is a lipid phosphatase that produce phosphatidylinositol 3,4-bisphosphate (PI(3,4)P2) from phosphatidylinositol 3,4,5-triphosphate […]

Tecovirimat hydrate (formerly ST246; SIGA246; ST-246; SIGA-246; POXX), the hydrated form of Tecovirimat which is a p37 envelope protein inhibitor, is a small synthetic antiviral drug approvd on 7/13/2018 for the treatment of smallbox infection.

Ehp inhibitor is a novel and potent inhibitor of EHP. Ehp is a new secreted Staphylococcus aureus protein that potently inhibits the alternative complement activation pathway. Ehp was identified through a genomic scan as an uncharacterized secreted protein from S. aureus, and immunoblotting of conditioned S. aureus culture medium revealed that the Ehp protein was […]

SR-3737, an amino pyrazole and indazole analog, is a potent JNK inhibitor but is non-selective for JNK3 (IC50 = 12 nM) and p38 (IC50 = 3 nM). c-Jun N-terminal kinase 3alpha1 (JNK3alpha1) is a mitogen-activated protein kinase family member expressed primarily in the brain that phosphorylates protein transcription factors, including c-Jun and activating transcription factor-2 […]

NOT AVAILABLE (CONTROLLED SUBSTANCE; Schedule I drugs under the Controlled Substances Act.). Cannabidiol (CBD; trade name: Epidiolex) is a phytocannabinoid discovered in 1940 and initially thought not to be psychoactive. It is one of at least 113 cannabinoids identified in hemp plants, accounting for up to 40% of the plant’s extract. Articles published in 2017 […]

Atabecestat HCl (formerly known as JNJ-54861911 HCl), the hydrochloride salt of Atabecestat, is a novel potent, oral, and brain-penetrant inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1), which is an enzyme that is up-regulated in Alzheimer’s disease. β-Secretase enzyme (BACE) inhibition has been proposed as a priority treatment mechanism for Alzheimer’s disease (AD), […]

Napsagatran hydrate is a novel and specific inhibitor of extrinsic and intrinsic thrombin generation which inhibits clot-bound and free (fluid-phase) thrombin.

Tezosentan (RO610612; Veletr; RO-610612) is a novel, non-selective and dual antagonist/inhibitor of endothelian (ETA/ETB) receptor (pA2s of 9.5, 7.7 for ETA and ETB) with the potential to be used for the treatment of congestive heart failure. Tezosentan acts as a vasodilator and was designed as a therapy for patients with acute heart failure. Tezosentan inhibits […]

Tedizolid phosphate disodium (DA-7157; TR-700; DA7157; TR700; torezolid; Sivextro) is the disodium salt of Tedizolid phosphate which is the phosphate ester prodrug of tedizolid. Tedizolid was approved in 2014 by FDA to treat acute bacterial skin and skin structure infections.