General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
scavenger receptor class B type I
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Dockendorff, C., et al. 2015. ACS Med. Chem. Lett.6, 375.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥98% (HPLC) |
| Quality Level | 100 |
| form | solid |
| potency | 6 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white to yellow |
| solubility | DMSO: 5 mg/mL |
| storage temp. | 2-8°C |
