LM10

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

选择性色氨酸 2, 3-双加氧酶 (TDO) 抑制剂（人和小鼠 TDO 的 IC50 值分别为 0.62 和 2 μM）。

LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). LM10 exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. LM10 reduces growth of TDO-expressing P815 mastocytoma tumors in mice.

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LM10 (160 mg/kg; p.o.) prevents the growth of TDO-expressing P815 tumor cells and promotes better rejection of control clone P815B cl1, which does not express TDO. LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile.LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity.The plasma concentration of LM10 after oral administration of 160 mg/kg/day is between 20 and 40 μg/mL (87-175 μM), a concentration about 40 times above the IC50 measured in the cellular assay performed with the physiological concentration of plasma tryptophan. Animal Model:DBA/2 mice (6-8 weeks)Dosage:160 mg/kg/day Administration:p.o.Result:Prevented the growth of TDO-expressing P815 tumor cells and promoted better rejection of control clone P815B cl1, which does not express TDO.

LM10 | LM 10 | LM-10

Others

Other Targets

TDO

Others-Field

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1316695-35-8

229.22

C11H8FN5

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (218.14 mM)

Fc2cc3ncc(/C=C/c1nnnn1)c3cc2

6-fluoro-3-[(E)-2-(1H-1,2,3,4-tetrazol-5-yl)ethenyl]-1H-indole

(-20℃)

With Ice Pack

≥ 2 years