28050-38-6Relevant articles and documents
Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands
Festa, Carmen,Renga, Barbara,D'Amore, Claudio,Sepe, Valentina,Finamore, Claudia,De Marino, Simona,Carino, Adriana,Cipriani, Sabrina,Monti, Maria Chiara,Zampella, Angela,Fiorucci, Stefano
, p. 8477 - 8495 (2015/01/09)
Nuclear and G-protein coupled receptors are considered major targets for drug discovery. FXR and GP-BAR1, two bile acid-activated receptors, have gained increasing consideration as druggable receptors. Because endogenous bile acids often target both receptor families, the development of selective ligands has been proven difficult, exposing patients to side effects linked to an unwanted activation of one of the two receptors. In the present study, we describe a novel library of semisynthetic bile acid derivatives obtained by modifications on the cholane scaffold. The pharmacological characterization of this library led to the discovery of 7α-hydroxy-5β-cholan-24-sulfate (7), 6β-ethyl-3α,7β-dihydroxy-5β-cholan-24-ol (EUDCOH, 26), and 6α-ethyl-3α, 7α-dihydroxy-24-nor-5β-cholan-23-ol (NorECDCOH, 30) as novel ligands for FXR and GP-BAR1 that might hold utility in the treatment of FXR and GP-BAR1 mediated disorders.
CO2 incubator ozone sterilization device
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, (2007/10/16)
PROBLEM TO BE SOLVED: To provide an apparatus that ensures sterilization of a COincubator, has no leakage of fed ozone gas to the outside, uniformly circulates ozone in a storage and constantly and continuously controls an ozone concentration.SOLUTION: The apparatus for ozone sterilization of a COincubator includes: a sterilization tent 1 with an airtight hole 8a for airtightly protruding a leading end part of a tube connection part 14a provided in the COincubator 11 to the outside and a discharge part 9a for discharging ozone gas to the outside, for covering the COincubator 11 airtightly; an ozone gas generator 18 for applying circulating sterilization to the inside and the outside of the COincubator 11 covered by the sterilization tent 1 by pressure-feeding the ozone gas to the tube connection part 14a; and an ozone gas neutralization unit 26 for neutralizing and eliminating the ozone gas discharged from the discharge part 9a.
Microwave-assisted synthesis and in vitro antibacterial activity of novel steroidal thiosemicarbazone derivatives
Zhao, Zhigang,Shi, Zhichuan,Liu, Min,Liu, Xingli
, p. 7730 - 7734 (2013/02/22)
Herein, we reported the synthesis of 16 novel steroidal thiosemicarbazone derivatives via the condensation of steroidal ketones and substituted thiosemicarbazides under solvent-free conditions using microwave irradiation. The yields obtained are in the ra
Potential Bile Acid Metabolites. 6. Stereoisomeric 3,7-Dihydroxy-5β-cholanic Acids
Iida, Takashi,Chang, Frederic C.
, p. 2966 - 2972 (2007/10/02)
New synthetic routes to the four possible 3,7-dihydroxy acids are described.The principal reactions involved were inversions with DMF and Me2SO-crown ether and reduction of 12-oxo tosylhydrazones.Inversion of 3α-tosylates by the Me2SO-crown ether method succeeded but that of the corresponding mesylates did not.A table of 1H NMR chemical shift reference data of monosubstituted methyl cholanates pertinent to bile acid characterization has been expanded.
