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1mg | ||
Other Sizes |
ln Vitro |
When compared to mIL-6R, vobarilizumab exhibits a preferential binding affinity for sIL-6R [2]. Recombinant hIL-6 interacts with recombinant hsIL-6R, however this interaction is blocked by vobarilizumab (0–10 nM) [3]. TF-1 cell growth is inhibited by vobarilizumab (0-100 nM) [3].
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ln Vivo |
In cynomolgus monkeys, vobarilizumab (0.4–10 mg/kg, intravenously) reduces hIL-6-induced inflammation[3]. In cynomolgus monkeys, vobarilizumab (0.4–10 mg/kg intravenously) has demonstrated long-term exposure through binding to serum albumin[3].
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Animal Protocol |
Animal/Disease Models: hIL-6-induced inflammation in cynomolgus monkey[3]
Doses: 0.4 mg/kg, 2 mg/kg, or 10 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: Inhibited the acute phase response parameters: plasma levels of C-reactive protein (CRP), fibrinogen and platelets. Animal/Disease Models: Cynomolgus monkeys[3] Doses: 0.4 mg/kg, 2 mg/kg, or 10 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: pharmacokinetic/PK parameters of Vobarilizumab dose (mg/kg) T1/2 dominant (day) AUCinf (μg/day/mL) CL (mL/day/kg) Vss (mL/kg) 0.4 (iv) 1.73 16.3 24.8 42.8 2 (iv) 5.0 193 10.4 53.7 10 (iv) 6.61 1136 9 82.7 |
References |
[1]. Kerschbaumer A, et al. Efficacy of pharmacological treatment in rheumatoid arthritis: a systematic literature research informing the 2019 update of the EULAR recommendations for management of rheumatoid arthritis. Ann Rheum Dis. 2020 Jun;79(6):744-759.
[2]. M. Van Roy, et al. FRI0021 Alx-0061, an anti-IL-6r nanobody® for therapeutic use in rheumatoid arthritis, demonstrates in vitro a differential biological activity profile as compared to tocilizumab. Ann Rheum Dis. 2013. 72 (3). [3]. Van Roy M, et al. The preclinical pharmacology of the high affinity anti-IL-6R Nanobody® ALX-0061 supports its clinical development in rheumatoid arthritis. Arthritis Res Ther. 2015 May 20;17(1):135. |
CAS # |
1628814-88-9
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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.