布拉地新钠盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetBucladesine sodiumCat. No.: HY-B0764CAS No.: 16980-89-5分式: CHNNaOP分量: 491.37作靶点: PKA; Phosphodiesterase (PDE)作通路: Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; Metabolic Enzyme/Protease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 H2O : 42 mg/mL (85.

2、48 mM)DMSO : 35.71 mg/mL (72.67 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.0351 mL 10.1756 mL 20.3513 mL5 mM 0.4070 mL 2.0351 mL 4.0703 mL10 mM 0.2035 mL 1.0176 mL 2.0351 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保

3、存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% sa

4、lineSolubility: 2.08 mg/mL (4.23 mM); Clear solution此案可获得 2.08 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.23 mM); Clear solutio

5、nPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.23 mM); Clear solution此案可获得 2.08 mg/mL (4.23 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L

6、20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Bucladesine sodium salt (Dibutyryl-cAMP sodium salt)种稳定的环 AMP (cAMP) 类似物，也 种选择性的 PKA活化剂，可提细胞内 cAMP 的平。Bucladesine sodium salt 也salt 具有抗炎活性，可于伤愈合不良。种磷酸酯 (PDE) 抑制剂。Bucladesine sodiumIC & Target PKA PDE体外研究 Both choline acetyltransferase (Ch

7、AT) and vesicular acetylcholine transporter (VAChT) mRNA increased approximatelyfourfold after treatment of PC12 cells with Bucladesine (dibutyryl cyclic AMP; dbcAMP). ChAT and PKA activity are alsoincreased by Bucladesine5.体内研究 Intrahippocampal infusion of Bucladesine into the CA1 region (male Albi

8、no-Wistar rats) can cause an improvement inspatial memory in maze task. Bilateral infusion of 10 M and 100 M Bucladesine leads to a significant reduction inescape latency and travel distance (showing an improvement in spatial memory). Bucladesine via activation of PKAand induction of cAMP/PKA pathwa

9、y improved spatial memory retention1.户使本产品发表的科研献 J Endocrinol. 2019 Sep 1. pii: JOE-19-0284.R2.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sharifzadeh, M., et al., Post-training intrahippocampal infusion of nicotine-bucladesine combination causes a synergistic en

10、hancement effect on spatialmemory retention in rats. Eur J Pharmacol, 2007. 562(3): p. 212-20.2. Mafune, E., M. Takahashi, and N. Takasugi, Effect of vehicles on percutaneous absorption of bucladesine (dibutyryl cyclic AMP) in normal and damagedrat skin. Biol Pharm Bull, 1995. 18(11): p. 1539-43.3.

11、Rundfeldt, C., et al., The stable cyclic adenosine monophosphate analogue, dibutyryl cyclo-adenosine monophosphate (bucladesine), is active in a modelof acute skin inflammation. Arch Dermatol Res, 2012.4. Salehi F, et al. Effect of bucladesine, pentoxifylline, and H-89 as cyclic adenosine monophosph

12、ate analog, phosphodiesterase, and protein kinase Ainhibitor on acute pain. Fundam Clin Pharmacol. 2017 Aug;31(4):411-419.5. Shimojo M, et al. The cholinergic gene locus is coordinately regulated by protein kinase A II in PC12 cells. J Neurochem. 1998 Sep;71(3):1118-26.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been