| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
B2R[1][2]
|
|---|---|
| ln Vitro |
When used as a pre-treatment 30 minutes prior to BK, fumaribant chloride (MEN16132 free base; 1 µM) consistently reduces BK-induced FGF-2 production and decreases BK-induced FGFR-1 phosphorylation[2]. Except for AKT in HUVEC, fumabant chloride suppresses the phosphorylation of FRSα, ERK1/2, and STAT3 (induced by BK; 1 μM; for 15 min)[2].
|
| ln Vivo |
When injected into the knee 30 minutes prior to λ-carrageenan, fumibant chloride (MEN16132 free base; 100 µg per knee) suppresses between 40 and 45 percent of carrageenan-induced joint discomfort and knee joint oedema[1].
|
| Cell Assay |
Cell Viability Assay[2]
Cell Types: human umbilical vein endothelial cells (HUVEC) Tested Concentrations: 1 μM Incubation Duration:Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h) Experimental Results: Produced a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation (without affecting FGFR -2 activities). |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats weighing 250-300 g[1]
Doses: 100 µg per knee Route of Administration: Injection into the knee; 30 min before λ-carrageenan Experimental Results: Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. decreased the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%. |
| References |
[1]. Claudio Valenti, et al. Fasitibant Chloride, a Kinin B₂ Receptor Antagonist, and Dexamethasone Interact to Inhibit Carrageenan-Induced Inflammatory Arthritis in Rats. Br J Pharmacol. 2012 Jun;166(4):1403-10.
[2]. Erika Terzuoli, et al. Bradykinin B2 Receptor Contributes to Inflammatory Responses in Human Endothelial Cells by the Transactivation of the Fibroblast Growth Factor Receptor FGFR-1. Int J Mol Sci. 2018 Sep 6;19(9):2638. [3]. Paola Cucchi, et al. MEN16132, a Novel Potent and Selective Nonpeptide Antagonist for the Human Bradykinin B2 Receptor. In Vitro Pharmacology and Molecular Characterization. Eur J Pharmacol. 2005 Dec 28;528(1-3):7-16. |
| Molecular Formula |
C36H49CL3N6O6S
|
|---|---|
| Molecular Weight |
800.23
|
| CAS # |
1157852-02-2
|
| Related CAS # |
Fasitibant free base;869939-83-3;Fasitibant chloride hydrochloride;869880-33-1
|
| SMILES |
CC1=CC(=NC2=C1C=CC=C2OCC3=C(C(=CC=C3Cl)S(=O)(=O)NC4(CCOCC4)C(=O)N5CCN(CC5)C(=O)[C@H](CCC[N+](C)(C)C)N)Cl)C.[Cl-]
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2496 mL | 6.2482 mL | 12.4964 mL | |
| 5 mM | 0.2499 mL | 1.2496 mL | 2.4993 mL | |
| 10 mM | 0.1250 mL | 0.6248 mL | 1.2496 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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