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| ln Vitro |
ADWX 1 (1,10 nM, 1 h) TFA inhibited the production of IL-2 and IFN-γ and selectively inhibited the activation of human CD4+ CCR7-T cells[2]. ADWX 1 (1,10 nM, 50 min) TFA reduced [Ca2+] in activated CD4+ CCR7-TCM cells of EAE rats[2]. ADWX 1 (1,10 nM, 1 h) TFA reduced NF-κB activation and preferentially inhibited the mRNA and protein expression of Kv1.3 in CD4+ CCR7-T cells of EAE rats stimulated by myelin basic protein (MBP)[2]. ADWX 1 (1,10 nM, 3 days) TFA inhibited the activation of Th17 cells in CD4+ CCR7-T cells but did not inhibit their differentiation[2].
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| ln Vivo |
ADWX 1 (100 μg/kg/day, subcutaneous injection, 3 days) improved the condition by inhibiting the production of IL-2 and IFN-γ and the proliferation of CCR7-TEM in experimental autoimmune encephalomyelitis (EAE) in Sprague-Dawley rats [2]. ADWX 1 (5/10 mg/kg, subcutaneous injection, 2 weeks) did not cause any behavioral or tissue pathological changes in rats (acute toxicity test) [2].
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| Cell Assay |
RT-PCR[2]
Cell Types: CD4+ CCR7- T cells from EAE rats. Tested Concentrations: 1, 10 nM, 10 nM. Incubation Duration: 1 hour. Experimental Results: Preferentially inhibited the expression of Kv1.3 gene mRNA. Western Blot Analysis [2] Cell Types: CD4+ CCR7- T cells from EAE rats Tested Concentrations: 1, 10 nM. Incubation Duration: 1 hour. Experimental Results: Kv1.3 protein expression was preferentially inhibited. |
| Animal Protocol |
Animal/Disease Models:Stable symptoms of acute experimental autoimmune encephalomyelitis (EAE) were induced in Sprague-Dawley rats [2] via immunization.
Doses: 100 μg/kg/day for 3 consecutive days. Route of Administration: Subcutaneous injection (sc). Experimental Results: Neurological function scores were reduced on days 10, 11, 12, 13, and 14 compared to the vector control group. Inflammatory infiltration and demyelination of the affected spinal cord were significantly reduced. Production of IL-2 and IFN-γ was inhibited. High- and low-concentration myelin antigen-induced T cell proliferation was inhibited in a dose-dependent manner. CD4+CCR7-TEM cells were reduced. |
| References |
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| Molecular Formula |
C169H281N57O46S7.XC2HF3O2
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| Molecular Weight |
4071.85 (free base)
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| Related CAS # |
ADWX 1
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| Sequence |
Val-Gly-Ile-Asn-Val-Lys-Cys-Lys-His-Ser-Arg-Gln-Cys-Leu-Lys-Pro-Cys-Lys-Asp-Ala-Gly-Met-Arg-Phe-Gly-Lys-Cys-Thr-Asn-Gly-Lys-Cys-His-Cys-Thr-Pro-Lys (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34)VGINVKCKHSRQCLKPCKDAGMRFGKCTNGKCHCTPK (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34)
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| SequenceShortening |
VGINVKCKHSRQCLKPCKDAGMRFGKCTNGKCHCTPK (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34)
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| Appearance |
White to off-white solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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 Vitro) |
H2O : ≥ 100 mg/mL
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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.) |
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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