5.38769

Lipid Uptake Inhibitor, ML278

• Synonim(y): Lipid Uptake Inhibitor, ML278, 3,5-Dimethoxy-N-(4-(1-(2-methoxyacetyl)indolin-5-yl)thiazol-2-yl)benzamide, SR-BI inhibitor ML278
• Wzór empiryczny (zapis Hilla): C₂₃H₂₃N₃O₅S
• Numer CAS: 1604821-43-3
• Masa cząsteczkowa: 453.51
• Numer MDL: MFCD30532636
• Kod UNSPSC: 12352211
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Formularz: solid
• siła działania: 6 nM IC₅₀
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: light yellow
• rozpuszczalność: DMSO: 5 mg/mL
• temp. przechowywania: 2-8°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
scavenger receptor class B type I

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Inne uwagi

Dockendorff, C., et al. 2015. ACS Med. Chem. Lett.6, 375.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable