Icatibant (acetate) (Synonyms: HOE 140) |
| Catalog No.GC43888 |
L'icatibant (acétate) (acétate de HOE-140) est un antagoniste peptidique puissant et spécifique du récepteur de la bradykinine B2 avec une IC50 et un Ki de 1,07 nM et 0,798 nM respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 138614-30-9
Sample solution is provided at 25 µL, 10mM.
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Icatibant is a synthetic peptide antagonist of the bradykinin B2 receptor with IC50 and Ki values of 1.07 and 0.798 nM, respectively, in guinea pig ileal cell membranes. It inhibits bradykinin-induced contractions in isolated guinea pig ileum and pulmonary arteries as well as in rat uterus (IC50s = 11, 5.4, and 4.9 nM, respectively). In vivo, icatibant inhibits bronchoconstriction induced by bradykinin in a guinea pig model (ID50s = 13.4 and 31.8 pmol/kg, i.v., for pulmonary resistance and dynamic lung compliance, respectively). Icatibant (30 µg, i.v.) also reduces vascular permeability in the footpad and intestine in a mouse model of hereditary angioedema. Formulations containing icatibant have been used for the treatment of hereditary angioedema.
| Cas No. | 138614-30-9 | SDF | |
| Synonymes | HOE 140 | ||
| Canonical SMILES | O=C(N1[C@](CCCC2)([H])[C@]2([H])C[C@H]1C(N[C@H](C(O)=O)CCCNC(N)=N)=O)[C@@H]3N(C([C@H](CO)NC([C@H](CC4=CC=CS4)NC(CNC([C@@H]5C[C@@H](O)CN5C([C@H]6N(C([C@@H](NC([C@H](N)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCC6)=O)=O)=O)=O)=O)CC7=C(C=CC=C7)C3.OC(C)=O | ||
| Formula | C59H89N19O13S•XC2H4O2 | M.Wt | 1304.5 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | -20°C, protect from light |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7666 mL | 3.8329 mL | 7.6658 mL |
| 5 mM | 0.1533 mL | 0.7666 mL | 1.5332 mL |
| 10 mM | 0.0767 mL | 0.3833 mL | 0.7666 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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