TDI-10229

TDI-10229 is an inhibitor of soluble adenylyl cyclase (sAC, IC50 = 0.2 µM for the human enzyme in a cell-free assay). It is selective for sAC over the transmembrane ACs AC1-3, -5, -8, and -9 at 10 µM. TDI-10229 inhibits cAMP accumulation induced by the phosphodiesterase (PDE) inhibitor IBMX (Cay-13347) in rodent sAC-expressing HEK293 cells (IC50 = 0.1 µM). It also inhibits capacitation-induced cAMP accumulation and protein kinase A (PKA) activation in isolated mouse and human sperm when used at a concentration of 5 µM. TDI-10229 (5 and 50 µM) prevents the acrosome reaction and fertilization of mouse sperm with mouse oocytes in vitro.Formal Name: 4-chloro-6-[1,5-dimethyl-4-(phenylmethyl)-1H-pyrazol-3-yl]-2-pyrimidinamine. CAS Number: 2810887-45-5. Molecular Formula: C16H16ClN5. Formula Weight: 313.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 1 mg/ml. lambdamax: 213, 215 nm. SMILES: NC1=NC(Cl)=CC(C2=NN(C)C(C)=C2CC3=CC=CC=C3)=N1. InChi Code: InChI=1S/C16H16ClN5/c1-10-12(8-11-6-4-3-5-7-11)15(21-22(10)2)13-9-14(17)20-16(18)19-13/h3-7,9H,8H2,1-2H3,(H2,18,19,20). InChi Key: VSMTYSWGHKYXOF-UHFFFAOYSA-N.