DG-051

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 (Cay-20110). 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, Cay-11188), 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.Formal Name: (2S)-2-[[4-(4-chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoic acid, monohydrochloride. CAS Number: 929915-58-2. Molecular Formula: C21H24ClNO4 . HCl. Formula Weight: 426.3. Purity: >98%. Formulation: (Request formulation change), A solution in ethanol. Solubility: DMF: 20 mg/ml, DMSO: 12.5 mg/ml, Ethanol: 12.5 mg/ml, PBS (pH 7.2): 2 mg/ml. lambdamax: 231, 279 nm. SMILES: ClC1=CC=C(OC2=CC=C(OC[C@@H]3CCCN3CCCC(O)=O)C=C2)C=C1.Cl. InChi Code: InChI=1S/C21H24ClNO4.ClH/c22-16-5-7-19(8-6-16)27-20-11-9-18(10-12-20)26-15-17-3-1-13-23(17)14-2-4-21(24)25,/h5-12,17H,1-4,13-15H2,(H,24,25),1H/t17-,/m0./s1. InChi Key: UCPVOTSNNAVKNE-LMOVPXPDSA-N.