LIPID UPTAKE INHIBITOR ML278 (C005B-229702)

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

Molecular Weight: 453.51. Empirical Formula: C₂₃H₂₃N₃O₅S. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.

UPC:

12352211

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

5387690001