TC-SP 14

TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC₅₀ = 0.042 μM) with minimal activity at S1P3 (EC₅₀ = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge^[1]. IC50 & Target: EC₅₀: 0.042 μM (hS1P1), 3.47 μM (hS1P3)^[1] In Vitro: TC-SP 14 (compound 14) neither inhibits nor induces human cytochrome P450 enzymes, is nonmutagenic, and dose not significantly inhibit the hERG channel^[1]. In Vivo: TC-SP 14 (compound 14) (0-3 mg/kg, Orally, once) produces a dose-dependent reduction in circulating blood lymphocytes 24 h postdose^[1].
TC-SP 14 (0-3 mg/kg, Orally, daily for 10 days) significant reduces ovalbumin (OVA)-induced ear swelling^[1].
TC-SP 14 (2-15 mg/kg, IV or PO, once) possesses acceptable characteristics^[1].
Pharmacokinetic Parameters of TC-SP 14 in female Sprague-Dawley rats and male Cynomolgus ^[1].

species	rat	NHP
CL (L/h/kg)	0.33	0.50
Vss (L/kg)	3.3	1.6
T1/2 (h)	7.5	35.2
MRT (h)	10	3.3
% F	68	23