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60

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T28643	S1P1-IN-Ex26
	S1P1-IN-Ex26 is a potent, selective antagonist of S1P1 receptor.
T16833	S1P1 Agonist III	Others	Others
	S1P1 Agonist III is an effective and orally active S1P1 agonist (EC50: 18 nM).
T38716	SAR247799 SAR247799,S1P1 agonist 3
	SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4].
T79816	S1P1 agonist 6	LPL Receptor	GPCR/G Protein
	S1P1 agonist 6 (Compound I) 是一种可以通过阻断淋巴细胞迁移来减弱免疫反应的S1P1激动剂，常用于研究自身免疫性疾病的免疫抑制剂。
T62732	S1P1 agonist 5
	S1P1 agonist 5 是一种选择性的、口服具有活力的 S1P1 激动剂。S1P1 agonist 5 可以抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有潜力进行多发性硬化症 (MS) 的研究。
T61639	S1P1 agonist 4
	S1P1 agonist 4 在效价（EC50< 0.05 mg/kg）和预测人类半衰期方面都有更好的表现（t1/2 ～ 5 天）。
T79817	S1P1 agonist 6 hemicalcium	LPL Receptor	GPCR/G Protein
	S1P1 agonist 6 hemicalcium (Compound I) 为一S1P1激动剂，其通过抑制淋巴细胞迁移而降低免疫反应，适用于自身免疫性疾病研究中的免疫抑制剂。
T2026	CYM5442	S1P Receptor; LPL Receptor	GPCR/G Protein
	CYM5442 是高选择性和口服活性的鞘氨醇 1-磷酸受体激动剂，EC50为 1.35 nM。它激活依赖 S1P1的 p42/p44-MAPK 磷酸化，具有视网膜神经保护作用，可轻松穿过中枢神经系统。
T28169	NIBR-0213 NIBR 0213	LPL Receptor	GPCR/G Protein
	NIBR-0213 是S1P1选择性拮抗剂，有抗实验性自身免疫性脑脊髓炎的作用。在 GTPγ35S 试验中，它作用于人和大鼠S1P1的IC50分别为 2.0 nM 和 2.3 nM。
T3258	Ponesimod ACT-128800	S1P Receptor; LPL Receptor	GPCR/G Protein
	Ponesimod (ACT-128800) 是一种选择性 S1P1可口服激动剂，在放射性配体结合试验中的 IC50值为 6 nM。它可高效激活 S1P1介导的信号转导，EC50为5.7 nM。它可预防淋巴细胞介导的组织炎症，具有潜在的免疫调节活性。
T6403	Siponimod 辛波莫德,BAF-312	S1P Receptor; LPL Receptor	GPCR/G Protein
	Siponimod (BAF-312) 是有效，选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂，对 S1P1 和 S1P5 受体具有特异性，EC50 分别为 0.39 nM 和 0.98 nM。 BAF312 对 S1P1 和 S1P5 受体的特异性比 S1P2、S1P3 和 S1P4 受体高 1000 倍以上。
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。
T2171	SEW2871 SEW2871	S1P Receptor; LPL Receptor	GPCR/G Protein
	SEW 2871 是一种可口服的高选择性 S1P1激动剂，EC50为 13.8 nM。它减少血液中的淋巴细胞数量，可用于糖尿病、阿尔茨海默氏病、肝纤维化和炎症相关研究。它激活 ERK、Akt 和 Rac 信号通路，并诱导 S1P1 内在化和再循环。
T10305	Amiselimod hydrochloride MT-1303 hydrochloride	S1P Receptor; LPL Receptor	GPCR/G Protein
	Amiselimod hydrochloride (MT-1303 hydrochloride) 是一种鞘氨醇 1-磷酸受体 1 (S1P1) 调节剂。
TQ0227	Etrasimod APD334	S1P Receptor; LPL Receptor	GPCR/G Protein
	Etrasimod (APD334) 是一种特异性和口服的S1P1受体拮抗剂，在CHO 细胞中的IC50值为1.88 nM。
T22697	CS 2100 1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid	S1P Receptor	GPCR/G Protein
	CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) 是口服有活性 S1P3-sparingS1P1选择性激动剂，对人 S1P1的EC50值为 4.0 nM，对 HvGR 的ID50值为 0.407 mg/kg。它在大鼠体内具有免疫抑制作用。
T60204	W140 HBr	S1P Receptor	GPCR/G Protein
	[(3S)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid;hydrobromide 是一种S1P1拮抗剂，Ki=2.84 μM。
T7360	GSK2018682	S1P Receptor; LPL Receptor	GPCR/G Protein
	GSK2018682 是 1-磷酸鞘氨醇受体S1P1和S1P5激动剂，pEC50值分别为 7.7 和 7.2，可用于多发性硬化的研究。
T14924	Cenerimod ACT-334441	Others	Others
	Cenerimod (ACT-334441) is an agonist of sphingosine 1-phosphate 1 receptor (S1P1; EC50: 2.7 nM).
T15031	CYM50260	Others; LPL Receptor	GPCR/G Protein; Others
	CYM50260 是有效的、强选择性的鞘氨醇-1-磷酸 4 受体 (S1P4-R) 激动剂 (EC50= 45 nM)，对 S1P1-R，S1P2-R，S1P3-R 和 S1P5-R 无活性。
T10385	ASP-4058	S1P Receptor; LPL Receptor	GPCR/G Protein
	ASP-4058 是一种鞘氨醇磷酸受体 1 和 5 (S1P1 and S1P5) 的二代激动剂，具有选择性、安全性和口服活性。ASP-4058能改善小鼠实验性自身免疫性脑脊髓炎。
T4031	S1p receptor agonist 1 S1p-receptor-agonist-1	S1P Receptor; LPL Receptor	GPCR/G Protein
	S1p receptor agonist 1 (S1p-receptor-agonist-1) 是有口服活性的S1P 受体激动剂，具有诱导 S1P1 内化的活性，EC50为9.83 nM。它有潜力用于关节炎和实验性自身免疫性脑炎)的相关研究。
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)。
T15032	CYM50308	S1P Receptor; LPL Receptor	GPCR/G Protein
	CYM50308 是选择性和高亲和力的鞘氨醇-1-磷酸受体 4 激动剂，EC50为 56 nM。它对 S1P4-R 的选择性比 S1P5-R 高 37 倍。
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
T11372	GC7 Sulfate	Autophagy	Autophagy
	GC7 Sulfate 是 deoxyhypusine synthase(DHS)有效抑制剂。真核翻译起始因子5A2 (eIF5A2)是DHS 已知的底物，因此GC7通过抑制DHS 活性来抑制eIF5A2的激活。
T27459	GSK2263167 GSK-2263167,GSK 2263167
	GSK2263167 is an agonist of S1P1 receptor.
T41144	CYM5442 hydrochloride CYM 5442 hydrochloride
	CYM 5442 hydrochloride is a potent and selective S1P1agonistin vitro(EC50 = 1.35 nM). Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant.
T26962	CBP-307 CBP307
	CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator.
T27106	CYM50374
	CYM50374对Sphingosine-1-phosphate receptor 4（S1P4 ）具有抑制作用，IC50为 µM。
T71069	GSK1842799 HCl
	GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. Upon phosphorylation, GSK1842799 showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3. GSK1842799 demonstrated good oral bioavailability. On the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations, GSK1842799 was selected as a candidate for further clinical.
T32005	GSK1842799 GSK 1842799
	GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability.
T71564	GSK2018682 HCl
	GSK2018682 is a novel sphingosine-1-phosphate receptor 1 (s1p1) and 5 (s1p5) agonist.
T32006	GSK-2262167 sodium GSK-2262167,GSK2262167,GSK 2262167
	GSK-2262167 is a potent S1P1 agonist, as effective as fingolimod in collagen-induced arthritis models, and shows good preclinical pharmacokinetic properties.
T17237	VPC 23019	S1P Receptor; LPL Receptor	GPCR/G Protein
	VPC 23019是一种含芳基酰胺的鞘氨醇 1-磷酸(S1P)受体调节剂，S1P1和S1P3受体的竞争性拮抗剂，pKi 分别为7.86 和 5.93，S1P4和S1P5的激动剂，pEC50分别为 6.58 和 7.07。
T26557	ACT-209905 ACT 209905,ACT209905
	ACT-209905 is an agonist of S1P1 receptor.
T26867	BMS-986104 HCl BMS986104,BMS-986104,BMS 986104
	BMS-986104 is a potent and selective S1P1 receptor modulator.
T68678	VPC 24191
	VPC 24191 is a sphingosine 1-phosphate (S1P1/3) receptor agonist.
T31107	CS-0777 CS0777,CS 0777
	CS-0777 is a potent, selective, and orally active S1P1 agonist (sphingosine 1-phosphate receptor modulator).
T28385	PF-462991 PF-991,PF991,PF 991,PF 462991
	PF-462991 is a S1P1 agonist.
T71392	(R)-FTY-720 Vinylphosphonate
	(R)-FTY-720 Vinylphosphonate is a sphingosine 1-phosphate type 1 (S1P1) receptor agonist and lacks anti-apoptotic activity.
T12780L	RP-001 hydrochloride	Others	Others
	RP-001 hydrochloride is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
T12780	RP-001	Others	Others
	RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
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...
T29971	AMG-369 KB74649,KB 74649,AMG369,KB-74649
	AMG-369 (KB74649) is an effective S1P1/S1P5 dual agonist, with limited activity in S1P3, but no activity in S1P2/S1P4.
T62517	S1p receptor agonist 2
	S1p receptor agonist 2 (compound 1) 是一种 S1P5 受体的激动剂，选择性比 S1P1 和/或 S1P3 受体高。S1p receptor agonist 2 能够用于内源性 SIP 信号系统，以及减轻/预防中枢神经系统 (CNS) 疾病 (如神经退行性疾病) 的演技。
T21916	TC-SP 14
	TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen cha...
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.
T30529	BMS-520
	BMS-520 is a potent, selective S1P1 agonist that has shown impressive efficacy when administered orally in a rat model of arthritis and in a mouse model of experimental autoimmune encephalomyelitis (EAE) with multiple sclerosis.
T8840	PF-543 hydrochloride PF-543	Apoptosis; S1P Receptor; Autophagy; LPL Receptor	Apoptosis; Autophagy; GPCR/G Protein
	PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂，对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂，诱导细胞凋亡、坏死和自噬。

化合物

Cat.No: T28643

S1P1 Agonist III

Cat.No: T16833

Target: Others

Cat.No: T38716

Synonym: SAR247799,S1P1 agonist 3

S1P1 agonist 6

Cat.No: T79816

Target: LPL Receptor

S1P1 agonist 5

Cat.No: T62732

S1P1 agonist 4

Cat.No: T61639

S1P1 agonist 6 hemicalcium

Cat.No: T79817

Target: LPL Receptor

Cat.No: T2026

Target: S1P Receptor, LPL Receptor

Cat.No: T28169

Synonym: NIBR 0213

Target: LPL Receptor

Cat.No: T3258

Synonym: ACT-128800

Target: S1P Receptor, LPL Receptor

Cat.No: T6403

Synonym: 辛波莫德,BAF-312

Target: S1P Receptor, LPL Receptor

Cat.No: T6923

Synonym: 奥扎莫德,RPC-1063

Target: S1P Receptor, LPL Receptor

Cat.No: T2171

Synonym: SEW2871

Target: S1P Receptor, LPL Receptor

Amiselimod hydrochloride

Cat.No: T10305

Synonym: MT-1303 hydrochloride

Target: S1P Receptor, LPL Receptor

Cat.No: TQ0227

Synonym: APD334

Target: S1P Receptor, LPL Receptor

Cat.No: T22697

Synonym: 1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid

Target: S1P Receptor

Cat.No: T60204

Target: S1P Receptor

Cat.No: T7360

Target: S1P Receptor, LPL Receptor

Cat.No: T14924

Synonym: ACT-334441

Target: Others

Cat.No: T15031

Target: Others, LPL Receptor

Cat.No: T10385

Target: S1P Receptor, LPL Receptor

S1p receptor agonist 1

Cat.No: T4031

Synonym: S1p-receptor-agonist-1

Target: S1P Receptor, LPL Receptor

Ozanimod hydrochloride

Cat.No: T62552

Cat.No: T15032

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

Cat.No: T11372

Target: Autophagy

Cat.No: T27459

Synonym: GSK-2263167,GSK 2263167

CYM5442 hydrochloride

Cat.No: T41144

Synonym: CYM 5442 hydrochloride

Cat.No: T26962

Synonym: CBP307

Cat.No: T27106

Cat.No: T71069

Cat.No: T32005

Synonym: GSK 1842799

Cat.No: T71564

GSK-2262167 sodium

Cat.No: T32006

Synonym: GSK-2262167,GSK2262167,GSK 2262167

Cat.No: T17237

Target: S1P Receptor, LPL Receptor

Cat.No: T26557

Synonym: ACT 209905,ACT209905

Cat.No: T26867

Synonym: BMS986104,BMS-986104,BMS 986104

Cat.No: T68678

Cat.No: T31107

Synonym: CS0777,CS 0777

Cat.No: T28385

Synonym: PF-991,PF991,PF 991,PF 462991

(R)-FTY-720 Vinylphosphonate

Cat.No: T71392

RP-001 hydrochloride

Cat.No: T12780L

Target: Others

Cat.No: T12780

Target: Others

W140 (trifluoroacetate salt)

Cat.No: T38336

Synonym: W140 (trifluoroacetate salt)

Cat.No: T29971

Synonym: KB74649,KB 74649,AMG369,KB-74649

S1p receptor agonist 2

Cat.No: T62517

Cat.No: T21916

Cat.No: T41145

Cat.No: T30529

PF-543 hydrochloride

Cat.No: T8840

Synonym: PF-543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Cat. No.	Product Name	Target	Signaling Pathways
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。
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。

天然产物

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

Sphingosine-1-phosphate

Cat.No: T21500

Synonym: S1P

Target: Endogenous Metabolite, S1P Receptor, LPL Receptor

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