JTE-013

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JTE-013 是一种有效且特异性的 S1P2 拮抗剂。 JTE-013 抑制放射性标记的 S1P 与人和大鼠 S1P2 的特异性结合（IC50 分别：17 nM 和 22 nM）。JTE-013 是一种 S1P2 拮抗剂。 JTE-013（50-200 μM；1-3 天）降低细胞活力。

JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively).JTE-013 is a S1P2 antagonist. JTE-013 (50-200 μM;?1-3 days) decreased cell viability.?JTE-013 shows 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM.?JTE-013 (10-1000 nM;?30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.JTE-013 (gavage;?30 mg/kg daily for 14 consecutive days) decreases tumor size and tumor weight.?the modification of JTE-013 to produce the AB1 compound improved potency, intravenous pharmacokinetics, cellular activity, and antitumor activity in NB and may have enhanced clinical and experimental applicability.

JTE-013 (50-200 μM; 1-3 days) reduces cell viability. JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.JTE-013 displays 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM. Cell Viability AssayCell Line:SK-N-AS cells Concentration:50, 100, 150, 200 μ Incubation Time:1-3 days Result:Reduced cell viability.Western Blot Analysis Cell Line:SK-N-AS cells Concentration:10, 100, 1000 nM Incubation Time:30 mins Result:Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation.

JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight. Animal Model:Six-week-old female athymic NCr-nu/nu nude mice Dosage:30 mg/kg Administration:Gavage; daily for 14 consecutive days Result:Reduced tumor size and tumor weight.

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GPCR/G Protein

S1P Receptor

S1P2

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383150-41-2

408.29

C17H19Cl2N7O

>98% (HPLC)

DMSO:100 mg/mL (244.92 mM; Need ultrasonic)

CC(C1=C2C(N(C)N=C2C)=NC(NNC(NC3=CC(Cl)=NC(Cl)=C3)=O)=C1)C

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(-20℃)

With Ice Pack

≥ 2 years