AN15368 

AN15368 is an orally active trypanocidal agent and a prodrug of AN14667. AN15368 selectively targets CPSF3-mediated mRNA maturation in intracellular amastigotes of Trypanosoma cruzi, reducing the mRNA levels of the parasite. As a prodrug, AN15368 can be cleaved into its active carboxylate form by CBP of Trypanosoma cruzi. AN15368 completely clears long-term naturally acquired Trypanosoma cruzi infections in non-human primates. AN15368 can be used in the research of Chagas disease^[1].

AN15368 (2-fold serial dilutions; 48-72 h) potently inhibits growth of wild-type intracellular T. cruzi amastigotes with an IC₅₀ of 2.4 nM and wild-type extracellular T. cruzi amastigotes with an IC₅₀ of 5 nM^[1].
AN15368 (2-fold serial dilutions; 72 h) has reduced susceptibility in intracellular T. cruzi amastigotes overexpressing CPSF3, with an IC₅₀ of 11.8 nM, confirming CPSF3 as a target of AN15368^[1].
AN15368 (2-fold serial dilutions; 72 h) has drastically reduced susceptibility in intracellular T. cruzi amastigotes with the engineered Asn232His mutation in CPSF3, with an IC₅₀ of 0.5 μM, confirming CPSF3 as a target of AN15368^[1].
AN15368 (2-fold serial dilutions; 72 h) has drastically reduced susceptibility in intracellular T. cruzi amastigotes with disrupted TcCBP, with an IC₅₀ of 2.5 μM, confirming AN15368 requires activation by parasite serine carboxypeptidase^[1].
AN15368 (10 μM; 6 h) for epimastigotes, (50 nM) for amastigotes is converted to its active cleaved product AN14667 in wild-type T. cruzi epimastigotes and amastigotes, but not in TcCBP knockout parasites, confirming TcCBP mediates prodrug activation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AN15368 (10 mg/kg; p.o.; daily; 40 days) achieves sterile cure of Trypanosoma cruzi infection in C57BL/6J mice, with no detectable residual parasites after immunosuppression^[1].
AN15368 (1-5 mg/kg; p.o.; daily; 21 days) reduces Trypanosoma cruzi parasite load in hairless mice, with the 2.5 and 5 mg/kg doses achieving near-complete parasite suppression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

389.25

C₂₀H₂₈BNO₆

2152662-92-3

OB1OCC2=C1C(C)=C(C=C2)C(N[C@@H](C(C)C)C(OCC3CCOCC3)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Padilla AM, et al. Discovery of an orally active benzoxaborole prodrug effective in the treatment of Chagas disease in non-human primates. Nat Microbiol. 2022;7(10):1536-1546.  [Content Brief]