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Search Results for " sphingosine 1-phosphate (s1p) "

25

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6923 Ozanimod

奥扎莫德,RPC-1063

S1P Receptor; LPL Receptor GPCR/G Protein
Ozanimod (RPC-1063) 是一种选择性S1P1和S1P5受体激动剂,在[35S]-GTPγS 结合实验中,EC50分别为 410 pM 和 11 nM。它可研究治疗克罗恩病、溃疡性结肠炎、多发性硬化症和复发性多发性硬化症的试验。
T83910 S1PL-IN-31

Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31

S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM),同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内,S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中,由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平,并且在雌性大鼠中降低了心率。
T27864 LX-2931

LX 3305,LX2931,LX-3305,ACB20034,LX 2931,LX3305

S1P Receptor GPCR/G Protein
LX-2931(LX-3305) 是一种鞘氨醇-1-磷酸裂解酶(S1P)抑制剂,可用于治疗类风湿性关节炎。
T22102 ML-178

CYM50179

Others Others
ML-178 是一种二氯苯,是鞘氨醇-1-磷酸受体4(S1PR4)的强效选择性激动剂,EC50 为 46 nM,在25 μM 的浓度下对其他 S1P 受体没有影响。
T63047 SLP9101555

S1P Receptor; LPL Receptor GPCR/G Protein
SLP9101555 是一种有效且具有选择性的鞘氨醇激酶 2(SphK2)抑制剂,Ki 为90 nM。SLP9101555对SphK2具有很高的亲和力,是 SphK1 的 200 倍。SLP9101555 显著降低细胞外 S1P 鞘氨醇 1- 磷酸(S1P)水平。
T2539 Fingolimod hydrochloride

Fingolimod (FTY720) HCl,FTY720,盐酸芬戈莫德

TRP/TRPV Channel; S1P Receptor; PAK; LPL Receptor Cytoskeletal Signaling; GPCR/G Protein; Membrane transporter/Ion channel
Fingolimod hydrochloride (FTY720) 是一种新型免疫调节剂,是一种 1-磷酸鞘氨醇(S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它诱导 S1P1 的内化,从而抑制 S1P 活性。它被鞘氨醇激酶磷酸化,尤其是被 SK2 磷酸化,从而可与 S1PR1、3、4 和 5 结合
T14924 Cenerimod

ACT-334441

S1P Receptor GPCR/G Protein
Cenerimod (ACT-334441) 是一种具有口服活性、选择性和高效性的磷酸鞘氨醇 1 受体(S1P1)激动剂(EC50:1 nM)。Cenerimod 对多种 S1P 的亚型具有抑制作用,可用于研究鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。
T62552 Ozanimod hydrochloride

Ozanimod (RPC-1063) hydrochloride 是一种鞘氨醇 1-磷酸 (S1P) 受体调节剂,能够高亲和力地选择性结合 S1P 受体亚型 1 (S1P1) 和 S1P5 (S1P5)。Ozanimod hydrochloride 能够调节 hS1P1 受体 (EC50: 1.03 nM) 和 hS1P5 受体 (EC50: 8.6 nM)。Ozanimod hydrochloride 能够用于研究复发性多发性硬化 (MS)。
T38294 4-Deoxypyridoxine hydrochloride

S1P Receptor GPCR/G Protein
4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解,与 S1P 一样,减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T14930 Ceralifimod

ONO-4641

Others Others
Ceralifimod (ONO-4641) is a potent agonist for sphingosine 1-phosphate receptors 1 and 5 (EC50s: 27.3, 334 pM for human S1P receptor 1 and 5).
T36833 A6770

A6770 is an inhibitor of sphingosine-1-phosphate (S1P) lyase.1It induces accumulation of [3H]sphinganine-1-phosphate ([3H]dhS1P), an S1P lyase substrate, in IT-79MTNC3 cells that endogenously express high levels of S1P lyase (EC50= <0.01 μM), an effect that is reduced in the presence of vitamin B6(EC50= <100 μM). 1.Ohtoyo, M., Tamura, M., Machinaga, N., et al.Scintillation proximity assay to detect the changes in cellular dihydrosphingosine 1-phosphate levelsLipids51(10)1207-1216(2016)
T28838 SPM-242

SPM 242

SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat
T78160 SLB1122168 formic

LPL Receptor GPCR/G Protein
SLB1122168 formic为一种高效的Spns2介导的S1P释放抑制剂,其半抑制浓度(IC50)为94 nM。
T37955 Sphingosine-1-phosphate (d16:1)

Sphingosine-1-phosphate (d16:1)

C16 Sphingosine-1-phosphate (C16 S1P) is a derivative of sphingosine-1-phosphate that binds to S1P1/EDG-1, S1P3/EDG-3, and S1P2/EDG-5 receptors with affinities of 115%, 83%, and 103%, respectively, relative to S1P in CHO cells. C16 S1P was increased in postmortem primary open angle glaucoma trabecular meshwork samples.
T70613 SLP120701 HCl

SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T10387 ASP1126

Others Others
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist (EC50s: 7.12 nM, 517 nM for hS1P1 and hS1P3).
T70614 SLR080811 HCl

SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.
T70900 VT-ME6

VT-ME6 is a potent and selective sphingosine kinase 2 inhibitor. VT-ME6, contained a quaternary ammonium group as a warhead and established that a positively charged moiety is necessary for engaging key amino acid residues in the enzyme binding pocket.13,14 This compound is moderately potent (Ki = 8 lM) and displays three-fold selectivity for SphK2 over SphK1. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK...
T41145 TASP 0277308

TASP 0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP 0277308 inhibits S1P-induced chemotaxis (IC50 = 1.1-1.6 nM), HUVEC cell proliferation (IC50 = 3-3.6 nM) and suppresses angiogenesisin vivo. TASP 0277308 also blocks VEGF-induced tube-formation of HUVECsin vitroand reverses or impairs the development of arthritis or mechano-allodynia.
T71301 Opaganib HCl

ABC294640, also known as Opaganib, is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. Upon administration, ABC294640 competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. This may eventually lead to the induction of apoptosis a...
T64065 Siponimod hemifumarate

Siponimod (BAF-312) hemifumarate 是一种选择性的、有效的鞘氨醇 -1- 磷酸 (S1P) 受体调节剂。Siponimod hemifumarate 对 S1P1 受体 (EC50: 0.39 nM) 和 S1P5 受体 (EC50: 0.98 nM) 的选择性高于 S1P2 (EC50>10000 nM)、S1P3 (EC50>1000 nM) 和 S1P4 (EC50: 750 nM) 。Siponimod hemifumarate 能够用于研究多发性硬化症 (MS)。
T37548 azido-FTY720

azido-FTY720

FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Down-regulation of S1P1 recept...
T83893 SLB1122168

SLB1122168是Spns2的抑制剂,针对小鼠转运蛋白的IC50值为94 nM。该化合物在以10 mg/kg的剂量给药时,能降低循环中的淋巴细胞数量,但不影响小鼠的血浆S1P水平。
T38336 W140 (trifluoroacetate salt)

W140 (trifluoroacetate salt)

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 μM (2a = W146; 2b = W...
T37187 D-erythro/L-threo Lysosphingomyelin (d18:1)

D-erythro/L-threo Lysosphingomyelin (d18:1)

Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (O...

化合物

Ozanimod
Cat.No: T6923
Synonym: 奥扎莫德,RPC-1063
Target: S1P Receptor, LPL Receptor
S1PL-IN-31
Cat.No: T83910
Synonym: Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
Target:
LX-2931
Cat.No: T27864
Synonym: LX 3305,LX2931,LX-3305,ACB20034,LX 2931,LX3305
Target: S1P Receptor
ML-178
Cat.No: T22102
Synonym: CYM50179
Target: Others
SLP9101555
Cat.No: T63047
Synonym:
Target: S1P Receptor, LPL Receptor
Fingolimod hydrochloride
Cat.No: T2539
Synonym: Fingolimod (FTY720) HCl,FTY720,盐酸芬戈莫德
Target: TRP/TRPV Channel, S1P Receptor, PAK, LPL Receptor
Cenerimod
Cat.No: T14924
Synonym: ACT-334441
Target: S1P Receptor
Ozanimod hydrochloride
Cat.No: T62552
Synonym:
Target:
4-Deoxypyridoxine hydrochloride
Cat.No: T38294
Synonym:
Target: S1P Receptor
Ceralifimod
Cat.No: T14930
Synonym: ONO-4641
Target: Others
A6770
Cat.No: T36833
Synonym:
Target:
SPM-242
Cat.No: T28838
Synonym: SPM 242
Target:
SLB1122168 formic
Cat.No: T78160
Synonym:
Target: LPL Receptor
Sphingosine-1-phosphate (d16:1)
Cat.No: T37955
Synonym: Sphingosine-1-phosphate (d16:1)
Target:
SLP120701 HCl
Cat.No: T70613
Synonym:
Target:
ASP1126
Cat.No: T10387
Synonym:
Target: Others
SLR080811 HCl
Cat.No: T70614
Synonym:
Target:
VT-ME6
Cat.No: T70900
Synonym:
Target:
TASP 0277308
Cat.No: T41145
Synonym:
Target:
Opaganib HCl
Cat.No: T71301
Synonym:
Target:
Siponimod hemifumarate
Cat.No: T64065
Synonym:
Target:
azido-FTY720
Cat.No: T37548
Synonym: azido-FTY720
Target:
SLB1122168
Cat.No: T83893
Synonym:
Target:
W140 (trifluoroacetate salt)
Cat.No: T38336
Synonym: W140 (trifluoroacetate salt)
Target:
D-erythro/L-threo Lysosphingomyelin (d18:1)
Cat.No: T37187
Synonym: D-erythro/L-threo Lysosphingomyelin (d18:1)
Target:
Cat. No. Product Name Target Signaling Pathways
T21500 Sphingosine-1-phosphate

S1P

Endogenous Metabolite; S1P Receptor; LPL Receptor GPCR/G Protein; Metabolism
Sphingosine-1-phosphate (S1P) 是 S1P1-5 受体 (S1P1-5 receptors) 的激动剂和 GPR3、GPR6、GPR12 的配体。Sphingosine-1-phosphate 是细胞内的第二信使,动员 Ca2+ 作为 G 蛋白偶联受体的细胞外配体。Sphingosine-1-phosphate 是由鞘磷脂 (HY-113498) 或其他膜磷脂生成的重要脂质介质。
T7939 Fingolimod

2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇,FTY-720A,FTY-720,芬戈莫德

S1P Receptor; PAK; LPL Receptor Cytoskeletal Signaling; GPCR/G Protein
Fingolimod (FTY-720A) 是一种 1-磷酸鞘氨醇 (S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它还是pak1激活剂和免疫抑制剂。

天然产物

Sphingosine-1-phosphate
Cat.No: T21500
Synonym: S1P
Target: Endogenous Metabolite, S1P Receptor, LPL Receptor
Fingolimod
Cat.No: T7939
Synonym: 2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇,FTY-720A,FTY-720,芬戈莫德
Target: S1P Receptor, PAK, LPL Receptor
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