929915-58-2 Usage
Description
DG-051 is a potent, orally bioavailable leukotriene A4 hydrolase (LTA4H) inhibitor (Kd = 25 nM; IC50 = 47 nM), the enzyme that catalyzes the rate-determining step in the synthesis of LTB4 . However, it also inhibits the aminopeptidase activity of LTA4H with IC50 values of 72 and 150 nM when tested using the substrates L-alanine p-nitroanaline and prolyl-glycyl-proline peptide (PGP; ), respectively, potentially leading to PGP accumulation in vivo. DG-051 does not show any inhibitory activity against a panel of more than 50 additional aminopeptidases, ion channels, or HERG.
Uses
(2S)?-2-?[[4-?(4-Chlorophenoxy)?phenoxy]?methyl]?-1-?pyrrolidinebutanoic Acid Hydrochloride is a potent inhibitor leukotriene A4 hydrolase (LTA4H), which is a therapeutic target for developing treatments for cardiovascular diseases and cancers.
Check Digit Verification of cas no
The CAS Registry Mumber 929915-58-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,9,9,1 and 5 respectively; the second part has 2 digits, 5 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 929915-58:
(8*9)+(7*2)+(6*9)+(5*9)+(4*1)+(3*5)+(2*5)+(1*8)=222
222 % 10 = 2
So 929915-58-2 is a valid CAS Registry Number.
929915-58-2Relevant articles and documents
PROCESS FOR PREPARING 4- { (S) -2- (4-(4-CHLOROPHENOXY) PHENOXYMETHYL) PYRROLIDIN-1-YL) } BUTYRIC ACID AND SALTS THEREOF
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, (2011/02/24)
The present invention relates to a process for preparing 4-{(S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl}butyric acid and its salts.
Development of a scalable synthetic process for DG-051B, a first-in-class inhibitior of LTA4H
Enache, Livia A.,Kennedy, Isaac,Sullins, David W.,Chen, Wei,Ristic, Dragan,Stahl, Glenn L.,Dzekhtser, Sergey,Erickson, Robert A.,Yan, Changren,Muellner, Frank W.,Krohn, Michael D.,Winger, Jennifer,Sandanayaka, Vincent,Singh, Jasbir,Zembower, David E.,Kiselyov, Alex S.
experimental part, p. 1177 - 1184 (2010/04/22)
DG-051B is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack. Process optimization led from a linear seven-step synthetic procedure to a convergent
