TC-G 1006 |
| Catalog No.GC14532 |
S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1324003-64-6
Sample solution is provided at 25 µL, 10mM.
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S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.IC50 value: 18 nM(EC50) [1]Target: S1P1 agonistWhen dosed orally at 1 and 3 mg/kg, the azahydroxymethyl analogue 22 achieved statistically significant lowering of circulating blood lymphocytes 24 h postdose. In rats, a dose-proportional increase in exposure was measured when 22 was dosed orally at 2 and 100 mg/kg. 22 displayed excellent pharmacokinetic parameters with low clearance (CL = 0.11 L/h/kg), long mean residence time (40 h), and good oral bioavailability (F = 67%).
References:
[1]. Harrington PE, et al. Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core. ACS Med Chem Lett. 2011 Nov 23;3(1):74-8.
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