155561-67-4
Chemical Structure
PD151242
- CAS No.: 155561-67-4
- Formula:C34H45N5O6
- Molecular Weight:619.76
IUPAC Name: Na-((azepane-1-carbonyl)-L-leucyl)-1-methyl-D-tryptophyl-D-tyrosine
InChIKey: JVILFANCFWZBFU-ZGIBFIJWSA-N
SMILES: C([C@@H](NC([C@@H](NC(=O)N1CCCCCC1)CC(C)C)=O)C(N[C@H](CC2=CC=C(O)C=C2)C(O)=O)=O)C=3C=4C(N(C)C3)=CC=CC4
Biological Activity: PD151242 is a selective competitive antagonist of the endothelin ETA receptor, with KD values of 0.65 nM, 0.64 nM and 1.92 nM for human, rat and porcine receptors, respectively, and a KD value of 104 μM for the human ETβ receptor. When radiolabeled as [125I]-PD151242, PD151242 can be used to visualize and localize renal vascular ETA receptors[1][2].
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PD151242 | PD151242 is a selective competitive antagonist of the endothelin ETA receptor, with KD values of 0.65 nM, 0.64 nM and 1.92 nM for human, rat and porcine receptors, respectively, and a KD value of 104 μM for the human ETβ receptor. When radiolabeled as [125I]-PD151242, PD151242 can be used to visualize and localize renal vascular ETA receptors. | |||||||||||||||||||||
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References
- [1]. Davenport AP, et al. [125I]-PD151242: a selective ligand for endothelin ETA receptors in human kidney which localizes to renal vasculature. Br J Pharmacol. 1994;113(4):1303-1310. [Content Brief]
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[2]. Peter MG, Davenport AP. Selectivity of [125I]-PD151242 for human, rat and porcine endothelin ETA receptors in the heart. British journal of pharmacology. 1995 Jan;114(2):297.
