Lys-(Des-Arg9, Leu8)-Bradykinin (trifluoroacetate salt) (Synonyms: Des-Arg10,Leu9-Kallidin, Des-Arg10,Leu9-KD, LysLeu8Des-Arg9-BK, LysLeu8Des-Arg9-Bradykinin) |
| カタログ番号GC49916 |
ブラジキニンB1受容体拮抗剤
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Lys-(Des-Arg9, Leu8)-Bradykinin is a bradykinin B1 receptor antagonist (Ki = 0.43 nM for the rabbit aorta receptor).1 It is selective for the bradykinin B1 over the B2 receptor (Ki = >10 µM for the rabbit ileum receptor).2 Lys-(Des-Arg9, Leu8)-Bradykinin inhibits contractions induced by the bradykinin B1 receptor agonist Des-Arg9-bradykinin in isolated rabbit aortic rings (pA2 = 8.54).3 Intraperitoneal administration of Lys-(Des-Arg9, Leu8)-bradykinin (5 mg/kg per day for three days) reduces increases in paw edema in a rat model of arthritis induced by peptidoglycan-polysaccharide (PGPS).4
1.MacNeil, T., Bierilo, K.K., Menke, J.G., et al.Cloning and pharmacological characterization of a rabbit bradykinin B1 receptorBiochim. Biophys. Acta1264(2)223-228(1995) 2.Meini, S., Cucchi, P., Catalani, C., et al.Radioligand binding characterization of the bradykinin B2 receptor in the rabbit and pig ileal smooth muscleEur. J. Pharmacol.635(1-3)34-39(2010) 3.Drapeau, G., Audet, R., Levesque, L., et al.Development and in vivo evaluation of metabolically resistant antagonists of B1 receptors for kininsJ. Pharmacol. Exp. Ther.266(1)192-199(1993) 4.Blais, C., Jr., Couture, R., Drapeau, G., et al.Involvement of endogenous kinins in the pathogenesis of peptidoglycan-induced arthritis in the Lewis ratArthritis Rheum.40(7)1327-1333(1997)
| Cas No. | SDF | ||
| 同義語 | Des-Arg10,Leu9-Kallidin, Des-Arg10,Leu9-KD, LysLeu8Des-Arg9-BK, LysLeu8Des-Arg9-Bradykinin | ||
| Canonical SMILES | N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N1[C@H](C(N2[C@H](C(NCC(N[C@H](C(N[C@@H](CO)C(N3[C@H](C(N[C@@H](CC(C)C)C(O)=O)=O)CCC3)=O)=O)CC4=CC=CC=C4)=O)=O)CCC2)=O)CCC1)=O)=O.OC(C(F)(F)F)=O | ||
| Formula | C47H75N13O11 • XCF3COOH | M.Wt | 998.2 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 3 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0018 mL | 5.009 mL | 10.018 mL |
| 5 mM | 0.2004 mL | 1.0018 mL | 2.0036 mL |
| 10 mM | 0.1002 mL | 0.5009 mL | 1.0018 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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