Breceptine

Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer[1].

215713-39-6

B 9870

12352005

Bradykinin Receptor; ERK

GPCR/G Protein; MAPK/ERK Pathway; Stem Cell/Wnt

Cancer-Kinase/protease

Cancer

O=C([C@H]1N(C[C@H](O)C1)C([C@H]2N(CCC2)C([C@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC(CCCCCCC(N[C@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N3[C@@H](CCC3)C(N4[C@@H](C[C@@H](O)C4)C(NCC(N[C@@H](C5CC6=C(C=CC=C6)C5)C(N[C@@H](CO)C(N[C@H](C7CC8=C(C=CC=C8)C7)C(N9[C@]%10([H])[C@](CCCC%10)([H])C[C@H]9C(N[C@H](C(O)=O)CCCNC(N)=N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NCC(N[C@@H](C%11CC%12=C(C=CC=C%12)C%11)C(N[C@@H](CO)C(N[C@H](C%13CC%14=C(C=CC=C%14)C%13)C(N%15[C@]%16([H])[C@](CCCC%16)([H])C[C@H]%15C(N[C@H](C(O)=O)CCCNC(N)=N)=O)=O)=O)=O)=O

C136H200N38O28

2815.28

[1]Morissette G, et al. Antagonist, partial agonist and antiproliferative actions of B‐9870 (CU201) as a function of the expression and density of the bradykinin B1 and B2 receptors. British journal of pharmacology. 2007 Feb;150 (3) :369-79.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-P1650/

Reference compound1

No Development Reported

Bradykinin B1 Receptor (B1R) ; Bradykinin B2 Receptor (B2R) ; ERK1; ERK2