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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[1].

Product Specifications

CAS Number

229030-05-1

UNSPSC

12352209

Target

Endogenous Metabolite

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/r892.html

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

Molecular Formula

C58H83N13O12

Molecular Weight

1154.36

References & Citations

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

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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