NXT629 - PPAR Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENXT629Cat. No.: HY-114263CAS No.: 1454925-59-7分式: CHNOS分量: 609.78作靶点: PPAR作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (204.99 mM; Need ultrasonic)Mass Solvent1

2、 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6399 mL 8.1997 mL 16.3994 mL5 mM 0.3280 mL 1.6399 mL 3.2799 mL10 mM 0.1640 mL 0.8200 mL 1.6399 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；以下溶剂前的百分 指该溶剂在您配制终

3、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 (3.41 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 (3.41 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.41 mM); Clear solution1/2 Mas

4、ter of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 NXT629种有效、选择性、竞争性的 PPAR- 拮抗剂，对 PPAR 的 IC50 值为 77 nM，对其选择性于对其他核激素受体，如 PPAR，PPAR，Er，GR 和 TR，IC50 值分别为 6.0，15，15.2，32.5 和100 M 1。NXT629 具有效抗癌作，在动物模型试验中，能够抑制实验性癌细胞转移 2。IC50 & Target hPPAR hPPAR hPPAR ER77 nM (IC50) 6 M (IC50) 15 M (IC50) 1

5、5.2 M (IC50)GR32.5 M (IC50)体外研究 NXT629 (Compound 33) is a potent, selective PPAR- antagonist, with an IC50 of 77 nM for human PPAR,shows high selectivity over other nuclear hormone receptor, such as PPAR, PPAR, Er, GR and TR,IC50s are 6.0, 15, 15.2, 32.5 and 100 M, respectively 1. NXT629 also compet

6、itively inhibits moussePPAR, PPAR/ and PPAR, with IC50s of 2.3, 35.1, 6.9 M, resepctively 2.体内研究 NXT629 (Compound 33; 30 mg/kg, i.p.) exhibits good pharmacokinetics in mouse, and significantlydecreases Fgf21 (Fibroblast growth factor 21), a PPAR target gene in fasted mice 1.NXT629 has poor oral bioa

7、vailability in mice and rats. NXT629 (30 mg/kg, i.p., daily for 6 weeks) delaysgrowth of subcutaneous SKOV-3 tumors in nude mice, inhibits growth of subcutaneous B16F10 tumors inC57Bl/6 mice. NXT629 (30 mg/kg, i.p.) is weakly anti-angiogenic against FGF-induced angiogenesis.NXT629 (3, 30 mg/kg, i.p.

8、) inhibits experimental metastasis of B16F10 melanoma cells to the mouse lung 2.REFERENCES1. Bravo Y, et al. Identification of the first potent, selective and bioavailable PPAR antagonist. Bioorg Med Chem Lett. 2014 May15;24(10):2267-72.2. Stebbins KJ, et al. In vitro and in vivo pharmacology of NXT629, a novel and selective PPAR antagonist. Eur J Pharmacol. 2017 Aug15;809:130-140.McePdfHeightCaution: Product has not been fully validated for medical applicat