|S5002||Fingolimod (FTY720) HCl||69 mg/mL||69 mg/mL||69 mg/mL|
|S7176||SKI II||<1 mg/mL||61 mg/mL||61 mg/mL|
|S7177||PF-543||<1 mg/mL||93 mg/mL||93 mg/mL|
|S7952||Ozanimod (RPC1063)||<1 mg/mL||81 mg/mL||10 mg/mL|
|S8241||Ponesimod||<1 mg/mL||92 mg/mL||92 mg/mL|
|S7182||JTE 013||<1 mg/mL||81 mg/mL||34 mg/mL|
|S7174||ABC294640||<1 mg/mL||76 mg/mL||28 mg/mL|
|S7179||BAF312 (Siponimod)||<1 mg/mL||100 mg/mL||44 mg/mL|
- S1P Receptor阻害剤(8)
- 新S1P Receptor製品
Fingolimod (FTY720) HCl（フィンゴリモド、Gilenya）は、0.033nMのIC50によるスフィンゴシン1-リン酸（S1P）受容体拮抗剤です。
Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8).
SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.
D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).
PF-543 is a cell-permeant, selective sphingosine kinase 1 (Sphk1) inhibitor with Ki of 3.6 nM, >100-fold selective over SphK2.
(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; *P < 0.05, **P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.
Ponesimod(ACT-128800)は1種、活性をしている経口S1P1（sphingosine-1-phosphate receptor 1）免疫調製剤です。このEC50値は5.7 Nmです。
JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
ABC294640 is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2.
BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively.