PD123319
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PD123319是血管紧张素II受体的非肽类抑制剂，IC50值为34 nM[1]。
血管紧张素II（Ang II）在多种生理功能，尤其是在血管收缩中起作用。不同于以往的药物，作为Ang II或ACE形成的抑制剂，PD123319是血管紧张素II受体的拮抗剂。在大鼠肾上腺和脑结合实验中，PD123319具有抑制作用，IC50值分别为34 nM和210 nM。在微粒体结合实验中，PD123319阻止Ang II与牛球状带微粒制剂的结合，IC50值为6.9 nM。据报道，PD123319可以抑制环磷酸鸟苷的生成，增加前列腺素E2的产生。此外，PD-123319不影响Ang II对蛋白酪氨酸磷酸化或胸苷掺入的效应[1，2，3]。
参考文献：
[1] Blankley C J, Hodges J C, Klutchko S R, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. Journal of medicinal chemistry, 1991, 34(11): 3248-3260.
[2] Boulay G, Servant G, Luong T T, et al. Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Molecular pharmacology, 1992, 41(4): 809-815.
[3] Siragy H. Angiotensin II receptor blockers: review of the binding characteristics. The American journal of cardiology, 1999, 84(10): 3-8.
| Physical Appearance | A colorless oil |
| Storage | Store at -20°C |
| M.Wt | 508.61 |
| Cas No. | 130663-39-7 |
| Formula | C31H32N4O3 |
| Solubility | ≥22.4 mg/mL in DMSO; ≥104.2 mg/mL in H2O; ≥140 mg/mL in EtOH |
| Chemical Name | (6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridine-6-carboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C=CC(=C1)CN2C=NC3=C2CC(N(C3)C(=O)C(C4=CC=CC=C4)C5=CC=CC=C5)C(=O)O)N(C)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
人间充质干细胞 |
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溶解方法 |
该化合物在DMSO中的溶解度 > 10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
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反应时间 |
10μM、15天 |
|
应用 |
PD123319通过抑制细胞外信号调节激酶信号，抑制人间充质干细胞的成骨分化。 |
| 动物实验 [2]: | |
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动物模型 |
大鼠模型 |
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剂量 |
0.5或2 mg/kg /天、皮下注射6、10天 |
|
应用 |
在新生大鼠中，PD123319在低剂量下减弱高氧诱导的肺和心脏损伤。 |
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注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
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References: 1Matsushita, K., Wu, Y., Pratt, R. E. and Dzau, V. J. (2015) Blockade of angiotensin II type 2 receptor by PD123319 inhibits osteogenic differentiation of human mesenchymal stem cells via inhibition of extracellular signal-regulated kinase signaling. J Am Soc Hypertens. 9, 517-525 2Wagenaar, G. T., Sengers, R. M., Laghmani el, H., Chen, X., Lindeboom, M. P., Roks, A. J., Folkerts, G. and Walther, F. J. (2014) Angiotensin II type 2 receptor ligand PD123319 attenuates hyperoxia-induced lung and heart injury at a low dose in newborn rats. Am J Physiol Lung Cell Mol Physiol. 307, L261-272 |
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| 描述 | PD 123319是一种有效的和选择性的AT2（血管紧张素II）受体的拮抗剂，IC50值为34 nM。 | |||||
| 靶点 | AT2 receptor | |||||
| IC50 | 34 nM | |||||
质量控制和MSDS
- 批次:
化学结构
