New Small Molecules from MCE for February 2021

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Na_v1.1 channels positive modulator. Lu AE98134 also increases the activity of Na_v1.2 and Na_v1.5 channels but not of Na_v1.4, Na_v1.6 and Na_v1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Na_v1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.

Compound Screening Libraries

50 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research.

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.

Cell Signaling Pathway

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).

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.

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