| Description | Isatoribine(ANA245) free base is a potent TLR7 receptor agonist with anti-hepatitis C virus infection activity for the study of HCV infection. |
| In vivo | Isatoribine is a selective agonist of TLR7. In a proof-of-concept study, we found that once-daily 7-day treatment with intravenous Isatoribine 800 mg caused a significant (P = .001) reduction of plasma HCV RNA (mean, -0.76; range, -2.85 to +0.21 log(10) units) in otherwise untreated patients (n = 12) who were chronically infected with HCV. Viral load reduction occurred in patients infected with genotype 1 as well as non-genotype 1 HCV. The reduction of viral load was correlated with the induction of markers of a heightened immune antiviral state, including 2'-, 5'- oligoadenylate synthetase levels in whole blood. This treatment was well tolerated, with a low frequency of mild to moderate adverse events. In conclusion, systemic administration of the selective TLR7 agonist Isatoribine resulted in dose-dependent changes in immunologic biomarkers and a statistically significant antiviral effect with relatively few and mild side effects.[1] |
| Synonyms | Isatoribine free base, ANA 245, Immusine, ANA-245, Isatoribine, Isatoribine monohydrate, ANA245 |
| molecular weight | 316.29 |
| Molecular formula | C10H12N4O6S |
| CAS | 122970-40-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (142.27 mM) |
| References | 1. Horsmans Y, et al. Isatoribine, an agonist of TLR7, reduces plasma virus concentration in chronic hepatitis C infection. Hepatology. 2005 Sep;42(3):724-31. 2. Xiang AX, et al. Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine. Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40. 3. Kaushik D, et al. Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles. RSC Med Chem. 2021 May 14;12(7):1065-1120. 4. Bayes M, et al. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Nov;27(9):665-77. |