| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| ln Vitro |
Acetyl octaarginine strongly inhibited the chymotrypsin-like activity and caspase-like activity of purified rat skeletal muscle 20S proteasome, with IC50 values of 100 nM and 200 nM, respectively, and had a weak inhibitory effect on trypsin-like activity; this inhibitory activity remained stable at physiological saline concentrations [1]. Acetyl octaarginine (maximum concentration 8 μM; action time 5-30 minutes) inhibited the activity of purified human erythrocyte 26S proteasome and 20S/PA28 proteasome complex, but its inhibitory efficiency was lower than that of isolated 20S proteasome [1]. Acetyl octaarginine (concentration 30-60 μM; action time 2 hours) inhibited the chymotrypsin-like activity and caspase-like activity of proteasome in cultured HeLa cells, leading to the accumulation of ubiquitinated proteins, but had no significant effect on trypsin-like activity [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]. Acetyl octarginine (3.9-7.9 nmol; 16 h) inhibits the growth of Escherichia coli and Staphylococcus aureus. At a concentration of 7.9 nmol (incubation for 16 h), the bacterial survival rate drops to 60%, and at a concentration of 3.9 nmol (incubation for 16 h), the bacterial survival rate drops to 40% [4]. Acetyl octarginine can cause cell membrane damage and increased permeability in Escherichia coli and Staphylococcus aureus [4]. Acetyl octarginine (5-30 nmol; 24 h) inhibits the growth of HeLa human cancer cells in a concentration-dependent manner. At a concentration of 15 nmol (incubation for 24 h), the inhibition rate can reach up to 49% [4].
|
|---|---|
| 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.XC2H4O2
|
|---|---|
| Molecular Weight |
1267.50 (free base)
|
| Related CAS # |
Octaarginine; 148796-86-5; Octaarginine TFA
|
| Sequence |
Arg-Arg-Arg-Arg-Arg-Arg-Arg-ArgRRRRRRRR
|
| SequenceShortening |
RRRRRRRR
|
| Appearance |
White to off-white solid
|
| 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 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)
|
| 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.) |
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
