5.38769

Lipid Uptake Inhibitor, ML278

• Synonym(s): Lipid Uptake Inhibitor, ML278, 3,5-Dimethoxy-N-(4-(1-(2-methoxyacetyl)indolin-5-yl)thiazol-2-yl)benzamide, SR-BI inhibitor ML278
• Empirical Formula (Hill Notation): C₂₃H₂₃N₃O₅S
• CAS Number: 1604821-43-3
• Molecular Weight: 453.51
• UNSPSC Code: 12352211
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• potency: 6 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C

Description

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).

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable