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PD123319

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Catalog No.
B2206
血管紧张素AT2受体的拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,100.00
现货
5mg
¥ 900.00
现货
10mg
¥ 1,110.00
现货
25mg
¥ 2,320.00
现货
50mg
¥ 3,534.00
现货

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Background

PD123319 is a non-peptide inhibitor of angiotensin II receptor with IC50 value of 34nM [1].

Angiotensin II play roles in a variety of physiological functions. Among these, the most prominent is vascular contraction. Unlike previous drugs act as inhibitors of the formation of Ang II or ACE, PD123319 is an antagonist of angiotensin II receptor. PD123319 shows inhibition potency in both rat adrenal and brain binding assay with IC50 values of 34nM and 210nM, respectively. It is found to prevent Ang II from binding the bovine zona glomerulosa microsomal preparation with IC50 value of 6.9nM in the binding assay using microsome. In addition, it is reported that administration of PD123319 can suppress the generation of cyclic guanosine monophosphate and increase the production of prostaglandin E2. Besides that, administration of PD-123319 does not infiuence the effect of Ang II on protein tyrosine phosphorylation or thymidine incorporation [1, 2 and 3].

Reference:
[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.

Chemical Properties

Physical AppearanceA colorless oil
StorageStore at -20°C
M.Wt508.61
Cas No.130663-39-7
FormulaC31H32N4O3
Solubility≥22.4mg/mL in DMSO, ≥140 mg/mL in EtOH, ≥104.2 mg/mL in H2O
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
SDFDownload SDF
Canonical SMILESCC1=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验 [1]:

细胞系

人间充质干细胞

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。

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]:

动物模型

大鼠模型

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。

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。

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

生物活性

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

化学结构

PD123319