Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidinedione, monohydrochloride
Purity: ≥98%
Formula Markup: C9H11ClN4O2 / HCl
Formula Weight: 279.1
CAS Number: 183204-72-0
Notes: Tipiracil is an inhibitor of thymidine phosphorylase (IC50 = 35 nM).{40279} It is selective for thymidine phosphorylase over uridine phosphorylase (UPase), thymidine kinase (TK), orotate phosphoribosyltransferase (OPRTase), and dihydropyrimidine dehydrogenase (DPD; IC50s = > 1,000 µM for all). Tipiracil also inhibits the severe acute respiratory coronavirus 2 (SARS-CoV-2) endoribonuclease nsp15 (IC50 = 7.5 µM).{69593} It reduces the levels of SARS-CoV-2 spike glycoprotein, also known as the surface glycoprotein, in SARS-CoV-2-infected A549 lung cancer cells when used at a concentration of 50 µM. Tipiracil (1 µM) prevents the metabolism of the DNA synthesis inhibitor trifluorothymidine (Item No. 21366) in human liver extracts.{40279}. It increases the plasma levels and potentiates the cytotoxicity of trifluorothymidine in an AZ-521 gastric carcinoma mouse xenograft model when administered at an equimolar dose. Formulations containing tipiracil have been used in the treatment of metastatic colorectal and gastric cancers.
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