Vedolizumab |
| رقم الكتالوجGC34211 |
فيدوليزوماب هو جسم مضاد أحادي النسيلة IgG1 يستهدف α ؛ 4β ؛ 7 إنتيجرين لعلاج التهاب القولون التقرحي ومرض كرون ' ؛ ق.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 943609-66-3
Sample solution is provided at 25 µL, 10mM.
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Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
Vedolizumab does not bind to the majority of memory CD4+ T lymphocytes (60%), neutrophils, and most monocytes. The highest level of vedolizumab binding is to a subset (25%) of human peripheral blood memory CD4+ T lymphocytes that include gut-homing interleukin 17 T-helper lymphocytes. Vedolizumab also binds to eosinophils at high levels, and to naive T-helper lymphocytes, naive and memory cytotoxic T lymphocytes, B lymphocytes, natural killer cells, and basophils at lower levels; vedolizumab binds to memory CD4+ T and B lymphocytes with subnanomolar potency (EC50=0.3-0.4 nM). Vedolizumab selectively inhibits adhesion of α4β7-expressing cells to mucosal addressin cell adhesion molecule 1 (IC50=0.02-0.06 g/mL) and fibronectin (IC50=0.02 g/mL), but not vascular cell adhesion molecule 1[1].
Blockade of α4β7 receptors on T-lymphocytes has been shown to occur for several weeks after a single dose of vedolizumab. The drug concentration following the infusion has been shown to be dose related with a mean maximum concentration of 12.5 μg/mL in those receiving 0.5 mg/kg of vedolizumab and 52.0 μg/mL in those receiving 2 mg/kg. The serum half-life of these two doses is 9-12 days respectively and saturation of α4β7 receptors on T-lymphocytes is >90% at both 4-6 weeks following infusion. In a dose ranging study, the serum drug concentrations increase with increasing dose and when regular induction infusions are used (on day 1, 15, 29 and 85), the serum half-life is between 15 and 22 days across all groups[1].
[1]. Soler D, et al. The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrintherapeutic antibody in development for inflammatory bowel diseases. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75. [2]. Singh H, et al. Vedolizumab: A novel anti-integrin drug for treatment of inflammatory bowel disease. J Nat Sci Biol Med. 2016 Jan-Jun;7(1):4-9.
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Kinase experiment: |
Vedolizumab inhibition of high-affinity binding of MAdCAM-1 to human peripheral blood memory CD4+ T lymphocytes is tested. Peripheral blood (90 μL) is incubated with a saturating concentration (3 μg/mL) of MAdCAM-1-murine-Fc fusion protein and 4 mM MnCl2 in a final volume of 100 μL for 1 h at room temperature, in the presence or absence of vedolizumab. After washing with assay buffer, the cells are stained with fluorescentlabeled anti-mouse IgG for 15 min at room temperature. After washing again, cells are incubated with mouse serum for 10 min at room temperature, followed by staining with anti-CD4 and anti-CD45RO antibodies for 15 min at room temperature. After washing, red blood cells are lysed with BD FACS lysing solution and analyzed by flow cytometry in a FACSCalibur with CellQuest Pro software[1]. |
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References: [1]. Soler D, et al. The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrintherapeutic antibody in development for inflammatory bowel diseases. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75. |
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| Cas No. | 943609-66-3 | SDF | |
| Canonical SMILES | [Vedolizumab] | ||
| Formula | M.Wt | 146814.9 | |
| الذوبان | Soluble in DMSO | Storage | Store at -80°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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.0068 mL | 0.0341 mL | 0.0681 mL |
| 5 mM | 0.0014 mL | 0.0068 mL | 0.0136 mL |
| 10 mM | 0.0007 mL | 0.0034 mL | 0.0068 mL |
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Purity: >99.00%
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