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5.38769

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C23H23N3O5S
CAS Number:
Molecular Weight:
453.51
UNSPSC Code:
12352211

Assay

≥98% (HPLC)

Quality Level

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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