Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Kv1.3 1.89 pM (IC50) Kv1.1 0.65 nM (IC50)
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ln Vitro |
ADWX 1 (1, 10 nM, 1 h) suppresses human CD4+ CCR7-TEM cell activation only while lowering IL-2 and IFN-γ levels [2]. ADWX 1 (1, 10 nM, 50 min) lowers the levels of [Ca2+] in CD4+ CCR7- TCM cells that are activated and generated from EAE rats [2]. ADWX 1 (1, 10 nM, 1 h) specifically lowers Kv1.3 gene and protein levels and inhibits the activation of NF-κB in myelin basic protein (MBP)-activated CD4+ CCR7- T cells from EAE rats [2]. In CD4+ CCR7- T cells, ADWX 1 (1, 10 nM, 3 days) suppresses Th17 activation but not differentiation [2].
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ln Vivo |
ADWX 1 (100 μg/kg/day, SC, 3 days) suppresses the production of IL-2 and IFN-γ in addition to inhibiting CCR7-TEM in the experimental autoimmune encephalomyelitis (EAE) model of Sprague-Dawley rats. The illness is improved by cell proliferation [2]. In rats, ADWX 1 (5/10 mg/kg, oral, 2 weeks) did not cause alterations in behavior or tissue pathology (acute toxicity experiment) [2].
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Cell Assay |
RT-PCR[2]
Cell Types: CD4+ CCR7- T cells from EAE rats Tested Concentrations: 1, 10 nM Incubation Duration: 1 h Experimental Results: Suppressed Kv1.3 gene mRNA expression preferentially. Western Blot Analysis[2] Cell Types: CD4+ CCR7 - T cells from EAE rats Tested Concentrations: 1, 10 nM Incubation Duration: 1 h Experimental Results: Suppressed Kv1.3 protein expression preferentially. |
Animal Protocol |
Animal/Disease Models: Stable symptoms of acute experimental autoimmune encephalomyelitis (EAE) were induced by immunizing SD (Sprague-Dawley) rats[2].
Doses: 100 μg/kg/day, 3 days Route of Administration: subcutaneous (sc) injection Experimental Results: decreased neurological scores compared with vehicle-treated rats on days 10, 11, 12, 13 and 14. decreased in inflammatory infiltrates and demyelination in the affected spinal cord Dramatically. Inhibited IL-2 and IFN-γ productions. Inhibited the T cell proliferation triggered by high and low concentrations of myelin antigen in a dose-dependent manner. diminished CD4+ CCR7- TEM cells. |
References |
[1]. Han S, et al. Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease. J Biol Chem. 2008 Jul 4;283(27):19058-65.
[2]. Li Z, et al. Selective inhibition of CCR7(-) effector memory T cell activation by a novel peptide targeting Kv1.3 channel in a rat experimental autoimmune encephalomyelitis model. J Biol Chem. 2012 Aug 24;287(35):29479-94. |
Molecular Formula |
C169H281N57O46S7
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Molecular Weight |
4071.85
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.2456 mL | 1.2279 mL | 2.4559 mL | |
5 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL | |
10 mM | 0.0246 mL | 0.1228 mL | 0.2456 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.