PD-123319
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Cat.No：IP3010 Solarbio
CAS：130663-39-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥97%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > GPCR & G Protein > PD-123319
Product Information
| CAS | 130663-39-7 |
| Name | PD-123319 |
| Molecular Formula | C31H32N4O3 |
| Molecular Weight | 508.61 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥97% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00896427 |
| SMILES | O=C([C@@H]1CC2=C(N=CN2CC3=CC=C(N(C)C)C(C)=C3)CN1C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)O |
| Target Point | Angiotensin Receptor |
| Passage | GPCR & G Protein |
| Background | PD123319 is a potent and selective AT2 angiotensin II receptor antagonist. |
| Biological Activity | PD 123319是血管紧张素II受体拮抗剂，IC50为34 nM[1-4]。 |
| IC50 | 34nM(AT2 Receptor)[1] |
| In Vitro | PD 123319显示出在许多不同组织中区分AII受体的两个亚类。 125I-AII在牛肾上腺肾小球细胞的膜制剂中特异性标记AII的两类结合位点。第一类(DuP-753敏感)代表AII总结合位点的约85％，并且对DuP-753具有高亲和力(IC50为92.9nM)。 PD-123319对125I-AII与该位点的结合没有任何影响。第二类结合位点对PD-123319更敏感，IC50为6.9 nM，对DuP-753的亲和力低得多(IC50约为10 microM)[2]。 |
| Animal Experiment | 在16 SHR中研究了CBF自动调节的下限。 8只动物接受PD 123319，而8只作为对照。静脉内施用PD123319或盐水，并且在注射后和开始自动调节研究之前使BP稳定10分钟。随后通过将血液抽入注射器诱导出血性低血压。通过这种方式，BP逐步降低到可获得的最低水平。在整个研究中，CBF的测量间隔为10至15 mmHg。 |
| Data Literature Source | [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]. Boulay G，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. Mol Pharmacol. 1992 Apr;41(4):809-15 [3]. Estrup TM，et al. 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]. Brillante DG，et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6. |
| Unit | Bottle |
| Specification | 1mg 5mg |
PD123319是一种有效的，选择性AT2血管紧张素Ⅱ受体拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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