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S82039

SR-3306

源葉(MedMol) 97%
  • 英文名:
  • SR-3306
  • 別名:
  • N-(4-(3-(6-methylpyridin-3-yl)-1H-1,2,4-triazol-1-yl)phenyl)-4-(3-morpholinophenyl)pyrimidin-2-amine
  • CAS號:
  • 1128096-91-2
  • 分子式:
  • C28H26N8O
  • 分子量:
  • 490.5591
品牌貨號產(chǎn)品規(guī)格價格(RMB) 庫存(上海) 北京 武漢 南京 數(shù)量計量單位 加入購物車...
源葉(MedMol) S82039-5mg 97% ¥1500.00元 預計交期:2-3天 - - - EA 加入購物車
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參考文獻

質檢證書(COA)

摩爾濃度計算器

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  • 提示:詳情請下載說明書。
  • 產(chǎn)品描述: SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.
  • 靶點: JNK
  • 體外研究:
    The effect of SR-3306 or Tat-Sab on cell viability in response to oxidative stress is measured by an MTT assay. H9c2 cells treated with 100 μM H2O2/FeSO4 are ~40% viable, whereas the addition of 500 nM SR-3306 or 500 nM SR3562 to cells treated with 100 μM H2O2/FeSO4 increases viability to ~90%, and the addition of 10 μM Tat-Sab peptide to cells treated with 100 μM H2O2/FeSO4 increases viability to ~70% compared with 98% viability in untreated cells. Similar results are found for primary human cardiomyocytes
  • 體內研究:
    Administration of SR-3306 [10 mg/kg/day (s.c.) for 14 days] increases the number of tyrosine hydroxylase immunoreactive (TH+) neurons in the SNpc by 6-fold and reduces the loss of the TH+ terminals in the striatum relative to the corresponding side of 6-OHDA-lesioned rats that receive only vehicle (p<0.05). In addition, SR-3306 [10 mg/kg/day (s.c.) for 14 days] decreases d-amphetamine-induced circling by 87% compared to 6-hydroxydopamine (6-OHDA)-lesioned animals given vehicle. Steady-state brain levels of SR-3306 at day 14 are 347 nM, which is approximately 2-fold higher than the cell-based IC50 for this compound. Finally, immunohistochemical staining for phospho-c-jun (p-c-jun) reveals that SR-3306 [10 mg/kg/day (s.c.) for 14 days] produces a 2.3-fold reduction of the number of immunoreactive neurons in the substantia nigra pars compacta (SNpc) relative to vehicle treated rats. In lean mice, intraperitoneal (i.p.) or intracerebroventricular (i.c.v.) administration of SR-3306 reduces food intake and body weight. Moreover, i.p. and i.c.v. administrations of SR11935 exert similar anorectic effects as SR3306, which suggests JNK2 or JNK3 mediates aspect of the anorectic effect by pan-JNK inhibition. Furthermore, daily i.p. injection of SR-3306 (7 days) prevents the increases in food intake and weight gain in lean mice upon high-fat diet feeding, and this injection paradigm reduced high-fat intake and obesity in diet-induced obese (DIO) mice
  • 參考文獻:
    1. Crocker CE, et al. JNK Inhibition Protects Dopamine Neurons and Provides Behavioral Improvement in a Rat 6-hydroxydopamine Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Apr 20;2(4):207-212. 2. Gao S, et al. Pharmacological Inhibition of c-Jun N-terminal Kinase Reduces Food Intake and Sensitizes Leptin's Anorectic Signaling Actions. Sci Rep. 2017 Feb 6;7:41795. 3. Chambers JW, et al. Inhibition of JNK mitochondrial localization and signaling is protective against ischemia/reperfusion injury in rats. J Biol Chem. 2013 Feb 8;288(6):4000-11.
  • 溶解性: soluble  in  DMSO
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 2.038 ml 10.192 ml 20.385 ml
    5 mM 0.408 ml 2.038 ml 4.077 ml
    10 mM 0.204 ml 1.019 ml 2.038 ml
    50 mM 0.041 ml 0.204 ml 0.408 ml
  • 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。
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