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HPA-12

(Synonyms: (1R,3S)-HPA-12) 目录号 : GC45710

An inhibitor of CERT

HPA-12 Chemical Structure

Cas No.:383418-30-2

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5mg
¥4,625.00
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HPA-12 is a ceramide analog and inhibitor of ceramide transfer protein (CERT).[1],[2] It inhibits binding of a ceramide probe to the isolated steroidogenic acute regulatory protein-related lipid transfer (START) domain of CERT with an EC50 value of 4 μM in a TR-FRET assay.[2] HPA-12 (2.5 μM) inhibits conversion of the fluorescent ceramide analog C5-DMB-Cer to C5-DMB-sphingomyelin in CHO and HeLa cells.[1] It also inhibits sphingomyelin synthesis in wild-type, but not ATP-dependent ceramide transport-deficient, CHO cells when used at a concentration of 1 μM.

Reference:
[1]. Yasuda, S., Kitagawa, H., Ueno, M., et al. A novel inhibitor of ceramide trafficking from the endoplasmic reticulum to the site of sphingomyelin synthesis. J. Biol. Chem. 276(47), 43994-44002 (2001).
[2]. Santos, C., Fluery, L., Rodriguez, F., et al. The CERT antagonist HPA-12: First practical synthesis and individual binding evaluation of the four stereoisomers. Bioorg. Med. Chem. 23(9), 2004-2009 (2015).

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1 mg 5 mg 10 mg
1 mM 2.751 mL 13.7552 mL 27.5103 mL
5 mM 0.5502 mL 2.751 mL 5.5021 mL
10 mM 0.2751 mL 1.3755 mL 2.751 mL
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