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Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.
ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).
BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
Nature. 2021 Jan;589(7843):620-626. Cell. 2021 Jan 21;184(2):370-383.e13. Cell. 2021 Jan 21;184(2):521-533.e14. Nat Cell Biol. 2021 Jan;23(1):40-48. Cancer Cell. 2020 Dec 31; S1535-6108(20)30660-7.
