IDO-IN-7-NLG-919-analogue-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIDO-IN-7Cat. No.: HY-13983CAS No.: 1402836-58-1Synonyms: NLG-919 analogue; GDC-0919 analogue分式: CHNO分量: 282.38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

2、6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) Ethanol : 25 mg/mL (88.53 mM; Need ultrasonic)DMSO : 15 mg/mL (53.12 mM; Need warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.5413 mL 17.7066 mL 35.4133 mL5 mM 0.7083 mL 3.5413 mL 7.0827 mL10 mM 0.3541 mL 1.7707 mL 3.5413 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

3、儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.85 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility

4、: 2.5 mg/mL (8.85 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.85 mM); Clear solution4. 請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.85 mM); Clear solution5. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% (2

5、0% SBE-CD in saline)Solubility: 2.5 mg/mL (8.85 mM); Clear solution6. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (8.85 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 IDO-IN-7 (NLG-919 analogue)種有效的 IDO1 抑制劑, IC50為 38 nM。IC50 & Target IDO138 nM (IC50)體外研究 IDO-IN-7 (NLG-919 analogue) is a potent

6、 IDO1 inhibitor (IC50=38 nM). The binding mode of IDO-IN-7 toIDO1 is experimentally available and shows a direct coordinative interaction to the sixth coordination site offerric heme. IDO-IN-7 has been used as reference compound in other studies to validate high-throughputscreening assay for IDO1 in

7、hibition and develop immunostimulatory nanomicellar carrier 1.PROTOCOLCell Assay IDO-IN-7 (NLG-919 analogue) and the selected fragments 8, 15, and 18 are tested in cellular assay for theirability to cross cell membrane and inhibit IDO1 catalytic activity. The cell line of murine mastocytoma P1.HTRst

8、ably transfected with murine IDO1 (P1.IDO1) is cultured for 16 hrs in the presence of each compound atthe concentration of 30 mM. The ability of P1.IDO1 cells to convert LTrp contained in the culture medium atthe concentration of 78.4 M into L-Kyn is then assessed after 16 hrs of incubation 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Coletti A, et al. Fragment-based approach to identify IDO1 inhibitor building blocks. Eur J Med Chem. 2017 Dec 1;141:169-177.McePdfHeightCaution: Product has not been fully validated for medical a