| Bioactivity | GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection. |
| CAS | 878197-98-9 |
| Formula | C24H32N6O |
| Molar Mass | 420.55 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kilogram-Scale Synthesis of the CXCR4 Antagonist GSK812397 |