Lobradimil
Based on 1 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.76%
- CAS 番号: 159768-75-9
- 分子式: C49H75N15O12S
- 分子量:1098.28
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保管条件:
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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-17446
IcatibantBradykinin Receptor Antagonist -
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Allo-acaLeptin Receptor Antagonist Peptide -
HY-162874
diABZI-V/C-DBCOSTING Agonist -
HY-108896
Icatibant acetateBradykinin B2 Antagonist -
HY-139100B
m7G(5')ppp(5')A diammoniumCap Analog -
HY-P1278
GR 64349NK2 Receptor Agonist -
HY-15039
SSR240612 -
HY-N9319
Fulvotomentoside ATriterpenoid Saponin -
HY-141466A
Crotonyl-CoA tetrasodiumDerivative of CoA -
![Lys-[Des-Arg9]Bradykinin TFA](https://file.medchemexpress.com/product_pic/hy-103295a.gif)
HY-103295A
Lys-[Des-Arg9]Bradykinin TFABradykinin B1 Receptor Agonist
MedChemExpress（MCE）の使用を引用している文献 Lobradimil
MoreBradykinin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
Bradykinin B2 Receptor (B2R) 0.54 nM (Ki) |
体外実験
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. Further protocols information, click here.
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 159768-75-9
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性状 Solid
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分子量 1098.28
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分子式 C49H75N15O12S
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Color White to off-white
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別名
RMP 7
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-105155 関連分類
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