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MedChemExpress - Model Lobradimil - ...

MedChemExpress - Model Lobradimil - 159768-75-9

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].

Lobradimil

MCE China：Lobradimil

Brand：MedChemExpress (MCE)

Cat. No.HY-105155

CAS：159768-75-9

Synonyms：RMP 7

Purity：99.60%

Storage：Sealed storage, away from moisture and light, under nitrogen Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

IC50 & Target：Bradykinin B2 Receptor (B2R) 0.54 nM (Ki)

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。