iGOT1-01

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

iGOT1-01 是谷氨酸草酰乙酸转氨酶 1 (GOT1) 的有效抑制剂。在 GOT1/MDH1 测定和 GOT1/GLOX/HRP 测定中，iGOT1-01 的 IC50 分别为 84.6 μM 和 11.3 μM。 iGOT1-01可用于抗癌研究。

iGOT1-01 is an effective inhibitor of glutamate oxaloacetate transaminase 1(GOT1) . iGOT1-01 has IC50s of 84.6 μM and 11.3 μM in GOT1/MDH1 assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 can be used in anti-cancer studies.(In Vitro):iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM.(In Vivo):In female CD1 mice, iGOT1-01 (20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour ng/mL).

iGOT1-01 has an IC50 of 84.6 μM in the GOT1/MDH1 assay. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM. iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells.

iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL). Animal Model:Female CD1 mice with 9 weeks old Dosage:20 mg/kg (Pharmacokinetic Analysis)Administration:Oral Result:Has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL).

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Others

Other Targets

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882256-55-5

320.39

C19H20N4O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (312.12 mM)

O=C(N1CCN(C2=CC=CC3=C2C=CN3)CC1)NC4=CC=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years