| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Octarginine strongly inhibited the chymotrypsin-like and caspase-like activities of purified rat skeletal muscle 20S proteasomes, with IC50 values of 100 nM and 200 nM, respectively, and had a weak inhibitory effect on trypsin-like activities; this inhibitory activity remained stable at physiological saline concentrations [1]. Octarginine (concentration up to 8 μM; action for 5-30 minutes) inhibited the activity of purified human erythrocyte 26S proteasomes and 20S/PA28 proteasome complex, but its inhibitory efficiency was lower than that of isolated 20S proteasomes [1]. Octarginine (30-60 μM; action for 2 hours) inhibited the chymotrypsin-like and caspase-like activities of proteasomes in cultured HeLa cells, leading to the accumulation of ubiquitinated proteins, but had no significant effect on trypsin-like activities [1]. Free octarginine peptides can efficiently deliver proteins, peptides and plasmid DNA into cultured cells. Stearylation at the R8 position significantly improves the transfection efficiency of plasmid DNA, making it comparable to that of Lipofectamine [2]. Octarginine (3.9-7.9 nmol; 16 h) inhibits the growth of Escherichia coli and Staphylococcus aureus, with survival rates decreasing to 60% and 40%, respectively, at a concentration of 7.9 nmol (incubation for 16 h) [4]. Octarginine can cause cell membrane damage and increased permeability in Escherichia coli and Staphylococcus aureus [4]. Octarginine (5-30 nmol; 24 h) inhibits the growth of HeLa human cancer cells in a concentration-dependent manner, with the highest inhibition rate of 49% at a concentration of 15 nmol (incubation for 24 h) [4].
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|---|---|
| ln Vivo |
Rhodamine-labeled octargine (R8) (20 μL, 0.1 mM; intra-articular injection; single dose) showed the highest articular cartilage matrix binding efficiency among the polyarginine peptides tested [3]. Rhodamine-labeled octargine (R8) (20 μL, 0.1 mM; intra-articular injection; single dose) significantly reduced the accumulation of rhodamine in degenerated articular cartilage in CAIA mice, reflecting the loss of chondroitin sulfate proteoglycans [3].
|
| References |
|
| Molecular Formula |
C48H98N32O9
|
|---|---|
| Molecular Weight |
1267.50
|
| CAS # |
148796-86-5
|
| Sequence |
Arg-Arg-Arg-Arg-Arg-Arg-Arg-ArgRRRRRRRR
|
| SequenceShortening |
RRRRRRRR
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(C(=O)O)(F)F.O=C(C(CCC/N=C(\N)/N)NC([C@H](CCC/N=C(\N)/N)NC([C@H](CCC/N=C(\N)/N)NC([C@H](CCC/N=C(\N)/N)N)=O)=O)=O)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N
|
| 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 | 0.7890 mL | 3.9448 mL | 7.8895 mL | |
| 5 mM | 0.1578 mL | 0.7890 mL | 1.5779 mL | |
| 10 mM | 0.0789 mL | 0.3945 mL | 0.7890 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.
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