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(Hyp3,β-(2-thienyl)-Ala5,Tyr(Me)8-psi(CH2NH)Arg9)-Bradykinin trifluoroacetate salt

Names

[ CAS No. ]:
159768-75-9

[ Name ]:
(Hyp3,β-(2-thienyl)-Ala5,Tyr(Me)8-psi(CH2NH)Arg9)-Bradykinin trifluoroacetate salt

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.53

[ Molecular Formula ]:
C49H75N15O12S

[ Molecular Weight ]:
1098.28000

[ Exact Mass ]:
1097.54000

[ PSA ]:
454.41000

[ LogP ]:
0.79560

[ Index of Refraction ]:
1.702

Related Compounds