SML3652

TASP0277308

≥98% (HPLC)

• Synonym(e): (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
• Empirische Formel (Hill-System): C₂₃H₂₈Cl₂N₆O₃S
• CAS-Nummer: 945725-50-8
• Molekulargewicht: 539.48
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD25977006
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

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).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable