R892 

R892 is a selective and efficient bradyK_inin 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].

1154.36

C₅₈H₈₃N₁₃O₁₂

229030-05-1

Ac-Lys-Arg-Pro-Pro-Gly-{Phe<Me>}-Ser-{d-Nal}-Ile

Ac-KRPPG-{Phe<Me>}-SA-{d-Nal}-I

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kinin B1 receptor antagonists containing alpha-methyl-L-phenylalanine: in vitro and in vivo antagonistic activities