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Merck

SML3652

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C23H28Cl2N6O3S
分子量:
539.48
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

-10 to -25°C

生化/生理作用

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).

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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