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Lobradimil

CAS: 159768-75-9 F: C49H75N15O12S W: 1098.28

Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM
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Bioactivity 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].
Invitro 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:
Name Lobradimil
CAS 159768-75-9
Formula C49H75N15O12S
Molar Mass 1098.28
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [1]. Warren K, et al. Phase II trial of intravenous lobradimil and carboplatin in childhood brain tumors: a report from the Children's Oncology Group. Cancer Chemother Pharmacol. 2006 Sep;58(3):343-7. [2]. Elliott PJ, et al. Dissociation of blood-brain barrier permeability and the hypotensive effects of the bradykinin B2 agonist, RMP-7. Immunopharmacology. 1996 Jun;33(1-3):205-8. [3]. Doctrow SR, et al. The bradykinin analog RMP-7 increases intracellular free calcium levels in rat brain microvascular endothelial cells. J Pharmacol Exp Ther. 1994 Oct;271(1):229-37. [4]. Mackic JB, et al. Cereport (RMP-7) increases the permeability of human brain microvascular endothelial cell monolayers. Pharm Res. 1999 Sep;16(9):1360-5.