Lipid Uptake Inhibitor, ML278

Cell permeable: yes

Primary Target
scavenger receptor class B type I

Reversible: yes

Toxicity: Standard Handling (A)

A cell-permeable, non-toxic, indolinyl-thiazole based compound that acts as a highly potent, reversible inhibitor of lipid uptake via scavenger receptor class B type I (SR-BI; IC₅₀ = 6 nM). Shown to block the uptake of [³H] labeled cholesteryl oleate ester ([³H]CE) from [³H]CE-HDL (IC₅₀ = 7 nM). Exhibits high selectivity when tested against a panel of 67 different receptors and secondary targets (at 10 µM). Displays excellent stability in human plasma (99% remaining after 5 h, with 94% plasma protein bound) and mouse liver microsomes (75% remaining after 1 h).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Dockendorff, C., et al. 2015. ACS Med. Chem. Lett.6, 375.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany