SML3652
TASP0277308
≥98% (HPLC)
别名:
(R)-3,4-Dichloro-N-(1-(4-ethyl-5-(3-(4-methylpiperazin-1-yl)phenoxy)-4H-1,2,4-triazol-3-yl)ethyl)benzenesulfonamide, 3,4-Dichloro-N-[(1R)-1-[4-ethyl-5-[3-(4-methyl-1-piperazinyl)phenoxy]-4H-1,2,4-triazol-3-yl]ethyl]benzenesulfonamide, TASP 0277308, TASP-0277308
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关于此项目
经验公式（希尔记法）:
C23H28Cl2N6O3S
化学文摘社编号:
分子量:
539.48
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active, highly S1P1 subtype-selective sphingosine-1-phosphate (S1P) receptor antagonist with in vitro and in vivo efficacy.
TASP0277308 is an orally active, highly S1P1 subtype-selective sphingosine-1-phosphate (S1P) receptor antagonist (IC50 = 2.7/4.2 nM against 0.1 nM S1P for binding mouse/human S1P1; IC50 >8.7 μM for S1P2-5). TASP0277308 effectively inhibits S1P1-mediated GTPγS membrane binding, cAMP response and chemotaxis (IC50 = 7.8, 3.5, 15 nM, respectively, agianst 10 nM S1P; hS1P1-expressing HEK293 or CHO) and demonstrates in vivo efficacy in various animal disease models, including collagen-induced arthritis and tumor angiogenesis in mice (10-100 mg/kg bid po), as well as neuropathic pain in rats (0.6-3 mg/kg via acute po or ip, acute 30 nmol or daily 10 nmol intrathecal injection).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Sphingosine 1-Phosphate Receptor Subtype 1 as a Therapeutic Target for Brain Trauma
Journal of Neurotrauma, 35(13), 1452-1466 (2018)
Sphingosine-1-phosphate receptor 1 activation in astrocytes contributes to neuropathic pain
Proceedings of the National Academy of Sciences of the USA, 116(21), 10557-10562 (2019)
Targeting the S1P/S1PR1 axis mitigates cancer-induced bone pain and neuroinflammation
Pain, 158(9), 1733-1742 (2017)
Amelioration of collagen-induced arthritis by a novel S1P1 antagonist with immunomodulatory activities
Journal of immunology (Baltimore, Md. : 1950), 188(1), 206-215 (2012)
Luca Piali et al.
Pharmacology research & perspectives, 5(6) (2017-12-12)
Sphingosine-1-phosphate receptor 1 (S1P1 ) modulators sequester circulating lymphocytes within lymph nodes, thereby preventing potentially pathogenic autoimmune cells from exiting into the blood stream and reaching inflamed tissues. S1P1 receptor modulation may thus offer potential to treat various autoimmune diseases.
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