Lobradimil
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 159768-75-9
- Formula: C49H75N15O12S
- Molecular Weight:1098.28
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Bradykinin Receptor Isoforms
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Biological Activity
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Bradykinin B2 Receptor (B2R) 0.54 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RG2 glioma cells-implanted rats[2]
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Dosage:1.5-18 μg/kg
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Administration:i.v. infusion, 0.05 mL/min for 15min
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Result:Increased Carboplatin (HY-17393) uptake (up to 80%) into brain tumors in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 159768-75-9
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Appearance Solid
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Molecular Weight 1098.28
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Formula C49H75N15O12S
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Color White to off-white
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Synonyms
RMP 7
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Solvent & Solubility
H2O : ≥ 50 mg/mL (45.53 mM)
DMSO : 25 mg/mL (22.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO / H2O | 1 mM | 0.9105 mL | 4.5526 mL | 9.1051 mL | 22.7629 mL |
| 5 mM | 0.1821 mL | 0.9105 mL | 1.8210 mL | 4.5526 mL | |
| 10 mM | 0.0911 mL | 0.4553 mL | 0.9105 mL | 2.2763 mL | |
| 15 mM | 0.0607 mL | 0.3035 mL | 0.6070 mL | 1.5175 mL | |
| 20 mM | 0.0455 mL | 0.2276 mL | 0.4553 mL | 1.1381 mL | |
| H2O | 25 mM | 0.0364 mL | 0.1821 mL | 0.3642 mL | 0.9105 mL |
| 30 mM | 0.0304 mL | 0.1518 mL | 0.3035 mL | 0.7588 mL | |
| 40 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5691 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Lobradimil Related Classifications
HY-105155 Related Classifications
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