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Description
Overview
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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).
Form
Light yellow solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₃H₂₃N₃O₅S
Purity
≥98% by HPLC
Solubility
DMSO (5 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Dockendorff, C., et al. 2015. ACS Med. Chem. Lett.6, 375.