Telotristat Etiprate

Telotristat etiprate is a prodrug form of telotristat, which is an inhibitor of tryptophan hydroxylase 1 (TPH1). Telotristat etiprate (15-300 mg/kg) reduces levels of serotonin (5-HT, Cay-14332) in mouse jejunum and blood but not brain. It inhibits increases in IL-1beta and IL-6 levels, histological damage in the colon, and weight loss in a mouse model of trinitrobenzene sulfonic acid-induced colitis when administered at a dose of 200 mg/kg. In mice infected with the nematode T. muris, telotristat etiprate (300 mg/kg per day) reduces colonic levels of myeloperoxidase (MPO), IL-1beta, and IL-17, as well as worm burden. Formulations containing telotristat etiprate have been used in the treatment of diarrhea associated with carcinoid syndrome.Formal Name: 4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-L-phenylalanine, ethyl ester, compd. with N-benzoylglycine. CAS Number: 1137608-69-5. Synonyms: LX 1032 hippurate, LX 1606 hippurate. Molecular Formula: C27H26ClF3N6O3 . C9H9NO3. Formula Weight: 754.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 50 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 5 mg/ml. lambdamax: 242, 308 nm. SMILES: NC1=NC(O[C@@H](C(F)(F)F)C2=CC=C(Cl)C=C2N3N=C(C)C=C3)=CC(C4=CC=C(C[C@H](N)C(OCC)=O)C=C4)=N1.O=C(NCC(O)=O)C5=CC=CC=C5. InChi Code: InChI=1S/C27H26ClF3N6O3.C9H9NO3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37,11-8(12)6-10-9(13)7-4-2-1-3-5-7/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35),1-5H,6H2,(H,10,13)(H,11,12)/t20-,24?,/m0./s1. InChi Key: XSFPZBUIBYMVEA-BAHZNLOQSA-N.