| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Arg-PEG1-Tα-syn (0-10 μM, 48 hours) significantly promoted the reduction of α-synA53T in U251 cells, with a DC50 of 0.28 μM and a Dmax of 90.5% at a concentration of 5 μM [1]. Arg-PEG1-Tα-syn (1 μM, 0-72 hours) exerted an α-synA53T degradation effect over time in U251/α-synA53T cells [1]. Arg-PEG1-Tα-syn (1 μM, 48 hours) showed consistent α-syn degradation effects in U251/α-synWT, U251/α-synA53T, 293/α-synWT, 293/α-synA53T, SH-SY5Y/α-synWT, and SH-SY5Y/α-synA53T cells [1]. Arg-PEG1-Tα-syn-induced α-synA53T reduction effect can be reversed by MG132 but not by Chloroquine[1]. Arg-PEG1-Tα-syn (1 μM, 48 h) regulates α-synWT and α-synA53T in U251 cells via the E3 ubiquitin ligase UBR1 (UBR1, UBR2, UBR4 and UBR5 were knocked down using shRNA)[1]. Arg-PEG1-Tα-syn (0-5 μM, 48 h) protects SH-SY5Y cells overexpressing α-synWT or α-synA53T from toxicity induced by α-syn WT or A53T overexpression by reducing α-synA53T aggregation[1].
|
|---|---|
| ln Vivo |
Arg-PEG1-Tα-syn (mixed with OP50 bacteria at different concentrations, po, continuously treated from L1 larval stage to day 5 of adult) in the Caenorhabditis elegans NL5901 strain can aggregate with α-synuclein, significantly improve the morphology of nerve cell bodies and synapses, and partially restore dopaminergic neuronal dysfunction caused by α-synuclein pathology [1]. Arg-PEG1-Tα-syn (mixed with OP50 bacteria at concentrations of 0-10 μM, po, continuously treated from L1 larval stage to day 5 of adult) can effectively improve motor dysfunction caused by α-synuclein pathology in a dose-dependent manner. This effect has been confirmed in nematodes overexpressing human α-syn A53T and has shown good safety in the UM0020 strain and wild-type nematodes [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: U251/α-syn A53T cells Tested Concentrations: 1 μM Incubation Duration: 0, 12, 24, 48 and 72 h Experimental Results: Degraded the α-syn A53T as early as 12 h, reaching the peak at 48 h. Western Blot Analysis[1] Cell Types: U251/α-synWT, U251/α-synA53T, 293/α-synWT, 293/α-synA53T, SH-SY5Y/α-synWT and SH-SY5Y/α-synA53T cells Tested Concentrations: 1 μM Incubation Duration: 48 h Experimental Results: Triggered efficient reduction of α-syn WT or α-syn A53T. Western Blot Analysis[1] Cell Types: U251 cells (knocked down UBR1, UBR2, UBR4, and UBR5 separately using shRNA) Tested Concentrations: 1 μM Incubation Duration: 48 h Experimental Results: Induced the degradation of both α-syn A53T and α-syn WT in U251 cells, an effect that is markedly suppressed by UBR1 knockdown but barely affected by UBR2, UBR4, or UBR5 knockdown. Cell Viability Assay[1] Cell Types: SH-SY5Y cells (overexpressing α-syn WT or α-syn A53T) Tested Concentrations: 0, 1 and 5 μM Incubation Duration: 48 h Experimental Results: Significantly enhanced cell viability in α-syn WT cells at 5 μM and in α-syn A53T cells starting at 1 μM. Immunofluorescence[1] Cell Types: SH-SY5Y cells Tested Concentrations: 5 μM Incubation Duration: 48 h Experimental Results: Significantly reduced α-syn A53T aggregates. Reduced α-syn A53T aggregates. |
| Animal Protocol |
Animal/Disease Models: C. elegans UM0020 (A537 mutant) and C. elegans NL5901 (W.T.)[1]
Doses: 0, 5 and 10 μM Route of Administration: p.o., om the L1 larval stage to day-5 adulthood Experimental Results: Significantly rescued the locomotor deficits of UM0020 worms at day-1 and day-5 of adulthood, with a more pronounced effect at day-5. Significantly improved the locomotor performance of UM0020 worms at 1 μM. Animal/Disease Models: C. elegans UM0020 and C. elegans NL5901 (W.T.)[1] Doses: 5 μM Route of Administration: p.o., om the L1 larval stage to day-5 adulthood Experimental Results: Has no significant difference in thrashing frequency. |
| References |
| Molecular Formula |
C22H29N7O2S
|
|---|---|
| Molecular Weight |
455.58
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1950 mL | 10.9750 mL | 21.9500 mL | |
| 5 mM | 0.4390 mL | 2.1950 mL | 4.3900 mL | |
| 10 mM | 0.2195 mL | 1.0975 mL | 2.1950 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
