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抑制剂描述:

产品名称:LM10

产品别名:见爱必信官网

英文别名:LM10

靶点:Others

CAS:1316695-35-8

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Selective tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P815 mastocytoma tumors in mice. Orally bioavailable.

溶解性:DMSO :45 mg/mL (196.33 mM)

体外研究:

LM10 (Ki=5.6 μM) displays an excellent selectively prolfile and does not display any inhibitory potency on IDO.

体内研究:LM10 has high plasma concentration and oral bioavailability in mouse. 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. Systemic treatment of immunized mice with LM10 at 160 (mg/kg)/day prevents the growth of TDO-expressing P815 tumor cells. Moreover, mice treated with LM10 do not show obvious signs of toxicity.

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