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CAS No.: 136676-91-0

PD 123319 ditrifluoroacetate Catalog No. CSN16875

Synonyms: PD 123319 (trifluoroacetate salt);PD-123319;PD-123319 TFA

PD123319 Ditrifluoroacetate is a potent, selective and non-peptide angiotensin AT2 receptor antagonist.

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技术信息

生物活性

描述PD 123319 (Ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM^[2]. Anaesthetised and ventilated SHR (spontaneously hypertensive rats) were given PD 123319, 0. 36 mg/kg/min, intravenously, and compared with a control group. PD 123319 did not influence baseline CBF (cerebral blood flow), but resulted in a minor BP (blood pressure) decrease^[3]. Further, 125I-All specifically labeled two classes of binding sites for All in a membrane preparation of bovine adrenal glomerulosa cells. PD-123319 did not have any effect on 125I-All binding to this site. The second class of binding sites was more sensitive to PD-123319, with an IC₅₀ of 6. 9 +/- 3. 7 nM, and had a much lower affinity for DuP-753 (IC₅₀ around 10 mM)^[4].
参考文献

[1] Blankley CJ, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60.
[2] Blankley CJ, Hodges JC, Klutchko SR, Himmelsbach RJ, Chucholowski A, Connolly CJ, Neergaard SJ, Van Nieuwenhze MS, Sebastian A, Quin J 3rd, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60.
[3] Estrup TM, Paulson OB, Strandgaard S. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92.
[4] Boulay G, Servant G, Luong TT, Escher E, Guillemette G. 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. Mol Pharmacol. 1992 Apr;41(4):809-15.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.3575 mL
- 6.7874 mL
- 13.5748 mL
- 5 mM
- 0.2715 mL
- 1.3575 mL
- 2.7150 mL
- 10 mM
- 0.1357 mL
- 0.6787 mL
- 1.3575 mL

技术信息

CAS号

136676-91-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C35H34F6N4O7

运输

蓝冰

分子量

736.66

别名

PD 123319 (trifluoroacetate salt);PD-123319;PD-123319 TFA

溶解度

DMSO	130.0 mg/mL (176.5 mM)
Water	70.0 mg/mL (95.0 mM)

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