VTX-27 _PKC 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVTX-27Cat. No.: HY-112782CAS No.: 1321924-70-2分式: CHClFNO分量: 418.9作靶点: PKC作通路: Epigenetics; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (298.40 mM; Need ultrasoni

2、c)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3872 mL 11.9360 mL 23.8720 mL5 mM 0.4774 mL 2.3872 mL 4.7744 mL10 mM 0.2387 mL 1.1936 mL 2.3872 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下

3、溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.97 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.97 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.97 mM); Clear

4、 solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 VTX-27蛋激酶 C (PKC ) 的选择性抑制剂，其对 PKC 和 PKC 的 Ki 值分别为 0.08 nM 和 16 nM。IC50 & Target PKC PKC PKC0.08 nM (Ki) 16 nM (Ki) 356 nM (Ki)体外研究 VTX-27 (Compound 27) possesses excellent overall characteristics. Good selectivity of VT

5、X-27 is also seenagainst other PKC family members, particularly classical isoforms (1000-fold except PKC I, 200-fold) andatypical isoforms (10000-fold). As anticipated, attaining selectivity over the more closely related novel PKCfamily members is more challenging, with a good 200-fold being achieve

6、d over PKC 1.体内研究 VTX-27 shows the best PK profile with a low clearance (7 mL min-1 kg-1), long half-life (4.7 h), and good oralbioavailability (65%). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at25 mg/kg Cmax concentration 700 ng/mL) and demonstrates poten

7、t dose dependent inhibition of IL-2production 1.REFERENCES1. Jimenez JM, et al. Design and optimization of selective protein kinase C (PKC) inhibitors for the treatment of autoimmune diseases. JMed Chem. 2013 Mar 14;56(5):1799-810.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use