BMS-986165 - TYK2 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBMS-986165Cat. No.: HY-117287CAS No.: 1609392-27-9分式: CHDNO分量: 425.46作靶點: JAK; Interleukin Related作通路: Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt;Immunology/Inflammation儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1

2、month溶解性數(shù)據(jù)體外實驗 DMSO : 62.5 mg/mL (146.90 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3504 mL 11.7520 mL 23.5040 mL5 mM 0.4701 mL 2.3504 mL 4.7008 mL10 mM 0.2350 mL 1.1752 mL 2.3504 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依?/p>

3、添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.89 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.89 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master

4、 of Small Molecules 您邊的抑制劑師www.MedChemE物活性 BMS-986165種效選擇性的，服物可利的 TYK2 變構(gòu)抑制劑，于治療免疫性疾病，BMS-986165 選擇性結(jié)合 TYK2 假激酶 (JH2) 結(jié)構(gòu)域 (IC50=1.0 nM)，并通過穩(wěn)定調(diào)節(jié) JH2 結(jié)構(gòu)域來阻斷受體介導(dǎo)的Tyk2 激活。BMS-986165 抑制 IL-12/23 和 I 型 IFN 途徑 1 2。IC50 & Target Tyk2 JH2 JAK1 JH20.2 nM (IC50) 1 nM (IC50)體外研究 BMS-986165 is differentiated fro

5、m previous JAK inhibitors due its unique ability to selectively bind to thepseudokinase (JH2) domain of TYK2 and inhibit its function through an allosteric mechanism 1.BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM,respectively) and shows no significant hE

6、RG inhibition in the flux assay (IC5080 M) 1.REFERENCES1. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of theAllosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18.2. Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase2. Annals of the Rheumatic Diseases 2017;76:859.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.