CRT0273750

Research use only, not for human use.

CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 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