CRT0273750

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

CRT0273750 调节血浆 LPA 水平，适用于体内研究。 CRT0273750 是一种自分泌运动因子 (ATX) 抑制剂，IC50 为 0.014 μM。

CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 0.014 μM.(In Vitro):CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM. CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM).(In Vivo):CRT0273750 treatment shows the Cmax, AUC and t1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively and shows a proportional increase.CRT0273750 has a moderate blood clearance, with value of 41 mL/min/kg.

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Animal Model:CD-1 mice Dosage:1 mg/kg Administration:I.v.Result:Had a moderate blood clearance.Animal Model:Balb-c nu/nu mice Dosage:10, 30 and 100 mg/kg Administration:Oral administration (Pharmacokinetic Analysis)Result:The Cmaxs were 3.8, 10.9 and 18.1 μM, respectively. The AUCs were 3.2, 15.2 and 59.3 μM.h, respectively.The t1/2s were 1.4, 0.9 and 1.3 h, respectively.

CRT 0273750 | CRT-0273750

Angiogenesis

PDE

Cannabinoid Receptor

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1979939-16-6

502.92

C25H22ClF3N4O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (497.10 mM)

C[C@H](NC(=O)CCc1nc2cccnc2n1Cc1ccc(OC(F)(F)F)cc1)c1ccc(Cl)cc1

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(-20℃)

With Ice Pack

≥ 2 years