GSK 1842799 TFA is a selective modulator of the S1P1 receptor, primarily developed for the treatment of multiple sclerosis (MS). The phosphorylated derivative, GSK1842799-P, demonstrates subnanomolar agonist activity for S1P1, with over 1000-fold selectivity against S1P3. This compound exhibits favorable pharmacokinetics, including good oral bioavailability and rapid in vivo conversion, leading to significant lymphocyte count reduction at a dose of 0.1 mg/kg. In preclinical models, it showcased comparable efficacy to FTY720, supporting its potential utility in MS research and other immune-related conditions.
GSK 1842799 TFA is a selective modulator of the S1P1 receptor, primarily developed for the treatment of multiple sclerosis (MS). The phosphorylated derivative, GSK1842799-P, demonstrates subnanomolar agonist activity for S1P1, with over 1000-fold selectivity against S1P3. This compound exhibits favorable pharmacokinetics, including good oral bioavailability and rapid in vivo conversion, leading to significant lymphocyte count reduction at a dose of 0.1 mg/kg. In preclinical models, it showcased comparable efficacy to FTY720, supporting its potential utility in MS research and other immune-related conditions.
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