Biological Activity
Selective, high affinity angiotensin AT2 receptor ligand (Ki = 0.24 nM). Displays agonistic properties at proximal tubule AT2 receptors, causes Na+, K+-ATPase inhibition and sodium excretion. Antagonizes Ang-II induced contractions in rabbit aortic rings (IC50 = 1850 nM).
Technical Data
| M. Wt | 1052.2 |
| Formula | C52H69N13O11 |
| Sequence |
YKHPI (Modifications: Tyr-1 = N-α-Nicotinoyl, Lys-2 = Lys-(N-α-Z-Arg)) |
| Storage | Desiccate at -20°C |
| CAS Number | 127060-75-7 |
| PubChem ID | 123794 |
| InChI Key | UXGNARZDONUMMK-LRMQDCNJSA-N |
| Smiles | CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](CCCCNC(=O)[C@H](CCCNC(N)=N)NC(=O)OCC1=CC=CC=C1)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)C1=CN=CC=C1)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1052.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.95 mL | 4.75 mL | 9.5 mL |
| 5 mM | 0.19 mL | 0.95 mL | 1.9 mL |
| 10 mM | 0.1 mL | 0.48 mL | 0.95 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.19 mL |
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References
References are publications that support the products' biological activity.
Naveri (1995) The role of angiotensin receptor subtypes in cerebrovascular regulation in the rat. Acta.Physiol.Scand.Suppl. 630 1 PMID: 8610501
Hakam and Hussain (2006) Angiotensin II AT2 receptors inhibit proximal tubular Na+-K+-ATPase activity via a NO/cGMP-dependent pathway. Am.J.Physiol.Renal Physiol. 290 F1430 PMID: 16380464
Criscione et al (1990) Binding characteristics and vascular effects of various angiotensin II antagonists. J.Cardiovas.Pharmacol. 16 S56 PMID:
Keywords: CGP 42112, supplier, Selective, high, affinity, AT2, ligands, Receptors, Angiotensin, CGP42112, Angiotensin, AT2, Receptors, Angiotensin, AT2, Receptors, Tocris Bioscience
