229030-05-1
Chemical Structure
R892
- CAS No.: 229030-05-1
- Formula:C58H83N13O12
- Molecular Weight:1154.36
IUPAC Name: ((R)-2-((S)-2-((S)-2-(2-((S)-1-(acetyl-L-lysyl-L-arginyl-L-prolyl)pyrrolidine-2-carboxamido)-N-methylacetamido)-3-phenylpropanamido)-3-hydroxypropanamido)-3-(naphthalen-2-yl)propanoyl)-L-isoleucine
InChIKey: QHTQATPXYIWRNI-JQUYBNPISA-N
SMILES: O=C([C@H]1N(CCC1)C([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCCN)=O)=O)N2[C@@H](CCC2)C(NCC(N(C)[C@H](C(N[C@@H](CO)C(N[C@@H](C(N[C@H](C(O)=O)[C@@H](C)CC)=O)CC3=CC4=CC=CC=C4C=C3)=O)=O)CC5=CC=CC=C5)=O)=O
Biological Activity: R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability[1].
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R892 | R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability. | |||||||||||||||||||||
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Keywords
