S1PR1
S1PR1 (sphingosine-1-phosphate receptor 1) is a G protein-coupled receptor that mediates cellular responses to sphingosine-1-phosphate (S1P) and plays essential roles in immune cell trafficking, endothelial homeostasis, vascular maturation, and cell migration.[1][2] Mechanistically, S1PR1 transduces extracellular S1P gradients into intracellular signaling programs that regulate lymphocyte egress from thymic and peripheral lymphoid tissues, thereby controlling immune surveillance and adaptive immune responses.[3][4] In vascular biology, S1PR1 signaling within endothelial cells is required for blood vessel stabilization, vascular smooth muscle cell coverage, and maintenance of endothelial barrier integrity, establishing a central role in vascular development and homeostasis.[1][2][5] Disease relevance of S1PR1 is strongly supported by studies in autoimmune and neuroinflammatory disorders, particularly multiple sclerosis, where dysregulated S1P-S1PR1 signaling contributes to pathological immune cell trafficking and tissue inflammation.[6][7] Compared with related S1P receptor isoforms, S1PR1 is distinguished by its dominant function in lymphocyte egress and vascular maturation, whereas other family members display partially distinct tissue distributions and signaling properties.[3][6] For experimental applications, selective S1PR1 modulators such as fingolimod-derived compounds induce receptor internalization and functional antagonism, reducing lymphocyte recirculation and providing valuable tools for investigating immune migration, endothelial signaling, and autoimmune disease mechanisms.[6][8]
References:
- [1]. Liu Y, et al. Edg-1, the G protein-coupled receptor for sphingosine-1-phosphate, is essential for vascular maturation. J Clin Invest. 2000 Oct;106(8):951-61. [Content Brief]
- [2]. Allende ML, et al. G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood. 2003 Nov 15;102(10):3665-7. [Content Brief]
- [3]. Matloubian M, et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature. 2004 Jan 22;427(6972):355-60. [Content Brief]
- [4]. Allende ML, et al. Expression of the sphingosine 1-phosphate receptor, S1P1, on T-cells controls thymic emigration. J Biol Chem. 2004 Apr 9;279(15):15396-401. [Content Brief]
- [5]. Prehoda KE. Microtubules in distress release arrest. Dev Cell. 2012 Aug 14;23(2):233-4. doi: 10.1016/j.devcel.2012.07.005. PMID: 22898771. et al. Microtubules in distress release arrest. Dev Cell. 2012 Aug 14;23(2):233-4. [Content Brief]
- [6]. Bravo GÁ, et al. Sphingosine-1-Phosphate (S1P) and S1P Signaling Pathway Modulators, from Current Insights to Future Perspectives. Cells. 2022 Jun 29;11(13):2058. [Content Brief]
- [7]. Ranganathan S, et al. Microbial 1-butanol production: Identification of non-native production routes and in silico engineering interventions. Biotechnol J. 2010 Jul;5(7):716-25. [Content Brief]
- [8]. Pan S, et al. A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol. 2006 Nov;13(11):1227-34. [Content Brief]
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S1PR1 Related Products (31)
Related Products (31)
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S1PR1 agonist 3
0 ImagesCat. No.: HY-178491CAS No.: 3028594-26-2S1PR1 agonist 3 (Compound Y18) is a highly selective S1PR1 receptor agonist (EC50=0.98 nM). S1PR1 agonist 3 is promising for research of autoimmune diseases such as multiple sclerosis and ulcerative colitis.
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BMS-520
0 ImagesCat. No.: HY-120615CAS No.: 1236188-38-7BMS-520 is a potent, orally active and selective sphingosine-1-phosphate 1 (S1P1) agonist with an EC50 of 0.47nM. BMS-520 shows ~3400-fold selectivity over S1P3. BMS-520 demonstrates impressive efficacy in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis. BMS-520 can be used for arthritis and EAE research.
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Udifitimod
0 ImagesCat. No.: HY-119245CAS No.: 1883345-06-9Synonyms: BMS-986166Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases.
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AMG 369
0 ImagesCat. No.: HY-14402CAS No.: 1202073-26-4AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat.
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TC-SP 14
0 ImagesCat. No.: HY-108492CAS No.: 1257093-40-5TC-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.
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S1PR1/S1PR5 agonist-1
0 ImagesCat. No.: HY-181875S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC50 values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease.
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CS-0777
0 ImagesCat. No.: HY-14976CAS No.: 827344-05-8CS-0777 is a selective, orally active sphingosine 1-phosphate receptor-1 modulator. CS-0777 can be used in the research of autoimmune diseases.
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CS1P1
0 ImagesCat. No.: HY-182626CAS No.: 1246526-29-3CS1P1 is a brain-penetrant and selective S1PR1 antagonist and PET radiotracer, with human S1PR1 IC50 values of 2.1 nM. CS1P1 binds specifically to S1PR1 to enable in vivo receptor expression quantification. CS1P1 can be used as PET radiotracer when labelled with 11C. CS1P1 can be used for the research of multiple sclerosis, neointimal hyperplasia, vascular inflammation.
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KRP-203 monophosphate
0 ImagesCat. No.: HY-182960CAS No.: 749262-82-6KRP-203 monophosphate is a monophosphate of KRP-203 (HY-13660). KRP-203 is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs.
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GSK-2262167 sodium
0 ImagesCat. No.: HY-18334CAS No.: 1165923-54-5GSK-2262167 sodium is a selective S1P1 receptor agonist. GSK-2262167 sodium is used for research on inflammatory and immune diseases.
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