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| 5mg | ||
| 10mg |
Vedolizumab (trade name Entyvio; Anti-Human lymphocyte α4β7 integrin, Humanized Antibody) is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease. Vedolizumab is a monoclonal antibody developed by Millennium Pharmaceuticals, Inc (a subsidiary of Takeda Pharmaceuticals) for the treatment of ulcerative colitis and Crohn's disease. It binds to integrin α4β7 (LPAM-1, lymphocyte Peyer's patch adhesion molecule 1). Blocking the α4β7 integrin results in gut-selective anti-inflammatory activity.
| ln Vitro |
Most monocytes, neutrophils, and 60% of memory CD4+ T cells are not bound by vedolizumab. A subset (25%) of human peripheral blood memory CD4+ T cells, including gut-homing interleukin 17 T-helper lymphocytes, exhibit the highest amount of vedolizumab binding. Vedolizumab also binds to basophils, naive T-helper lymphocytes, B lymphocytes, natural killer cells, naive and memory cytotoxic T lymphocytes, and eosinophils at high and low concentrations, respectively; it also binds to memory CD4+ T and B lymphocytes with subnanomolar potency (EC50=0.3-0.4 nM). Vedolizumab specifically prevents α4β7-expressing cells from adhering to fibronectin (IC50=0.02 μg/mL) and mucosal addressin cell adhesion molecule 1 (IC50=0.02-0.06 μg/mL), but not to vascular cell adhesion molecule 1[1].
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| ln Vivo |
It has been demonstrated that T-lymphocytes' α4β7 receptors remain blocked for several weeks following a single vedolizumab dosage. Following infusion, the drug concentration has been demonstrated to be dose-related, with a mean maximum concentration of 12.5 μg/mL in vedolizumab recipients getting 0.5 mg/kg and 52.0 μg/mL in recipients receiving 2 mg/kg. Both of these dosages have a serum half-life of 9–12 days, and after 4–6 weeks after infusion, T-lymphocyte α4β7 receptor saturation is greater than 90%. Serum drug concentrations rise with increasing dose in a dose-ranging research, and all groups' serum half-lives range from 15 to 22 days when frequent induction infusions are administered on days 1, 15, 29, and 85[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.
[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 |
| CAS # |
943609-66-3
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 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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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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