159768-75-9

159768-75-9 structure

Name: (Hyp3,β-(2-thienyl)-Ala5,Tyr(Me)8-psi(CH2NH)Arg9)-Bradykinin trifluoroacetate salt
Chemical Name: Lobradimil
CAS Number: 159768-75-9
Molecular Formula: C₄₉H₇₅N₁₅O₁₂S
Molecular Weight: 1098.28000
Catalog: Signaling Pathways GPCR/G Protein Bradykinin Receptor
Create Date: 2017-02-14 01:10:37
Modify Date: 2024-01-31 12:19:45
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors[1].

Name	Lobradimil
Synonyms	H-Arg-Pro-Hyp-Gly-b-(2-thienyl)-Ala-Ser-Pro-Tyr(Me)-()-Arg-OH LabradiMil,LabrodiMil,RMP-7,LobradiMil RMP 7 (Hyp3,b-(2-thienyl)-Ala5,Tyr(Me)8-()-Arg9)-Bradykinin

Description	Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor
Target	Bradykinin B2 Receptor (B2R):0.54 nM (Ki)
In Vitro	Lobradimil induces an increase in intracellular free calcium levels in RBME cells[3]. Lobradimil (0.01-0.5 nM, 15 min) increases the permeability of human brain microvascular endothelial cell (HMBEC) monolayers1[4].
In Vivo	Lobradimil (2.5-mg/kg bolus plus 10 mg/kg/h for 90 minutes) increases brain tumor permeability and shows hypotensive effects in RG2 glioma cells-implanted rats[2]. Animal Model: RG2 glioma cells-implanted rats[2] Dosage: 1.5-18 μg/kg Administration: i.v. infusion, 0.05 mL/min for 15min Result: Increased Carboplatin (HY-17393) uptake (up to 80%) into brain tumors in a dose-dependent manner.