DDD85646

DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki value of 1.44 nM. T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT. It less potently inhibits growth of T. cruzi (EC50 = 6.9 µM).Formal Name: 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide. CAS Number: 1215010-55-1. Synonyms: IMP-366. Molecular Formula: C21H24Cl2N6O2S. Formula Weight: 495.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/mL, DMSO: 25 mg/mL, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL, Ethanol: slightly soluble, PBS (pH 7.2): slightly soluble. lambdamax: 226, 258 nm. SMILES: ClC1=CC(C2=CC=NC(N3CCNCC3)=C2)=CC(Cl)=C1S(NC4=C(C)N(C)N=C4C)(=O)=O. InChi Code: InChI=1S/C21H24Cl2N6O2S/c1-13-20(14(2)28(3)26-13)27-32(30,31)21-17(22)10-16(11-18(21)23)15-4-5-25-19(12-15)29-8-6-24-7-9-29/h4-5,10-12,24,27H,6-9H2,1-3H3. InChi Key: XMBSZPZJLPTFMV-UHFFFAOYSA-N.