IDO5L - Indoleamine 2,3-Dioxygenase (IDO) 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIDO5LCat. No.: HY-15683CAS No.: 914471-09-3分式: CHClFNO分量: 271.64作靶點(diǎn): Indoleamine 2,3-Dioxygenase (IDO)作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 52 mg/mL

2、(191.43 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.6813 mL 18.4067 mL 36.8134 mL5 mM 0.7363 mL 3.6813 mL 7.3627 mL10 mM 0.3681 mL 1.8407 mL 3.6813 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 IDO5L種有效的吲哚胺-2,3-雙加氧酶 (IDO) 抑制劑

3、，IC50 為 67 nM。IC50 & Target IDO IDO67 nM (IC50) 19 nM (IC50, in HeLa cell)體外研究IDO5L (Compound 5l) is a potent (HeLa IC50=19 nM) inhibitor of IDO 1. IDO5L is one of the highest potent1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEinhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay) 2.體內(nèi)研究 Testin

4、g of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreasedkynurenine levels (50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t1/250(PBadjIC50=1.0

5、M, murine cellular B16 IC50=46 nM). Notably, kynurenine levels increase back to baselineafter 4 h as IDO5L exposure levels decreased below the mouse PBadjIC50 from 1.0 to 0.1 M 1.PROTOCOLAnimal Mice 1Administration 1 A single subcutaneous 100 mg/kg dose of IDO5L is administered to naive C57BL/6 mice

6、 bearing GM-CSF-secreting B16 tumors. Blood is harvested from individual mice over 8 h. Kynurenine and IDO5Lconcentrations are measured by LCMS. Reductions of kynurenine levels by 50-60% are observed between 2and 4 h, with maximum inhibition seen at 2.5 h. Tumors are allowed to grow until day 7 when

7、 14 days ofsubcutaneous dosing of IDO5L at 25, 50, and 75 mg/kg b.i.d. is initiated. Dose dependent inhibition of tumorgrowth is correlated with increasing exposures of IDO5L in plasma.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yue EW,

8、 et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity andefficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7.2. Huang X, et al. Synthesis of (18) F 4-amino-N-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): anovel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62.McePdfHeightCaution: Product has not been fully validated for medical appli