| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Hexa-D-arginine targets the proprotein convertase furin with high affinity (Ki = 106 nM). It also inhibits the related convertases PACE4 (Ki = 580 nM) and PC1 (Ki = 13.2 μM). By blocking furin, the peptide prevents the proteolytic activation of various bacterial toxins and viral glycoproteins, which is a critical step in their pathogenicity.
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|---|---|
| ln Vitro |
Hexa-D-arginine can effectively prevent cell lysis mediated by Pseudomonas aeruginosa exotoxin A (PEA) without being harmful by itself [1].
In vitro, Hexa-D-arginine effectively blocks Pseudomonas aeruginosa exotoxin A (PEA)-induced cell lysis and is itself noncytotoxic. It demonstrates potent inhibition of furin-mediated processes in cell-based assays without causing significant toxicity to the host cells. The peptide's activity is attributed to its ability to bind to the active site of furin and prevent substrate cleavage. |
| ln Vivo |
Hexa-D-arginine (0.1, 1, or 10 nM) administration was shown to reduce circulating TNF-α levels and enhance the survival rate of mice treated with Pseudomonas aeruginosa exotoxin A (PEA) (6-week-old FVB and 129/Sv mice)[1].
In vivo, Hexa-D-arginine has been shown to significantly improve the survival rate of PEA-treated mice while also reducing circulating levels of tumor necrosis factor-alpha (TNF-α). This indicates that the peptide can effectively block the lethal effects of bacterial toxins in a living organism, highlighting its potential as a therapeutic agent against furin-dependent pathogens. |
| Enzyme Assay |
In vitro non-cell enzyme assays for Hexa-D-arginine typically involve measuring the inhibition of furin, PACE4, and PC1 activity using purified enzymes and fluorogenic peptide substrates. The compound is incubated with the enzyme and substrate, and the rate of substrate cleavage is monitored by fluorescence. Ki values are calculated from steady-state kinetic analysis by fitting the data to appropriate inhibition models.
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| Cell Assay |
In vitro cell-based assays for Hexa-D-arginine use cell lines susceptible to furin-dependent toxins, such as those treated with Pseudomonas aeruginosa exotoxin A. Cells are pre-incubated with the peptide, followed by toxin exposure. Cell viability is assessed using standard assays like MTT or by measuring lactate dehydrogenase (LDH) release to quantify toxin-induced cell lysis. The peptide's lack of cytotoxicity is confirmed in parallel control experiments.
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| Animal Protocol |
In vivo animal studies for Hexa-D-arginine employ mouse models of toxin-induced lethality, such as challenge with Pseudomonas aeruginosa exotoxin A. The peptide is administered to the animals, and survival rates are monitored. Additionally, serum levels of inflammatory markers like TNF-α are measured to assess the compound's effect on the systemic inflammatory response.
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| ADME/Pharmacokinetics |
Hexa-D-arginine has a molecular weight of 954.14 g/mol and a molecular formula of C₃₆H₇₅N₂₅O₆. It is a white solid with a purity of ≥98%. The peptide is soluble in water at 100 mg/mL (104.8 mM) but is insoluble in DMSO. For storage, it should be kept dry, dark, and at -20°C for up to one year. As a hexa-arginine peptide, it is expected to have high water solubility and poor oral bioavailability due to its peptide nature.
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| Toxicity/Toxicokinetics |
Hexa-D-arginine is considered noncytotoxic in cell-based assays, indicating a favorable safety profile in vitro. In animal models, its administration has been shown to reduce circulating TNF-α levels, suggesting it may have a protective effect against the systemic inflammation caused by toxins. However, comprehensive toxicological studies are limited as the compound is primarily a research tool.
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| References | |
| Additional Infomation |
6-D-arginine is a peptide.
Hexa-D-arginine is a stable and specific furin inhibitor widely used as a research tool to study furin-mediated processes, including bacterial toxin activation and viral glycoprotein processing. It is also known as Furin Inhibitor II. The compound's ability to block toxin activation in vivo makes it a valuable lead compound for developing novel therapeutics against furin-dependent pathogens. It is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C36H75N25O6
|
|---|---|
| Molecular Weight |
954.1446
|
| Exact Mass |
953.633
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| CAS # |
673202-67-0
|
| Related CAS # |
Hexa-D-arginine TFA;958204-56-3
|
| PubChem CID |
57358476
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.303
|
| Hydrogen Bond Donor Count |
19
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| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
35
|
| Heavy Atom Count |
67
|
| Complexity |
1750
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| Defined Atom Stereocenter Count |
6
|
| SMILES |
C(C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(=O)N)N)CN=C(N)N
|
| InChi Key |
BMLTZEAFQLJTIZ-TZNXUKFXSA-N
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| InChi Code |
InChI=1S/C36H75N25O6/c37-19(7-1-13-51-31(39)40)26(63)58-21(9-3-15-53-33(43)44)28(65)60-23(11-5-17-55-35(47)48)30(67)61-24(12-6-18-56-36(49)50)29(66)59-22(10-4-16-54-34(45)46)27(64)57-20(25(38)62)8-2-14-52-32(41)42/h19-24H,1-18,37H2,(H2,38,62)(H,57,64)(H,58,63)(H,59,66)(H,60,65)(H,61,67)(H4,39,40,51)(H4,41,42,52)(H4,43,44,53)(H4,45,46,54)(H4,47,48,55)(H4,49,50,56)/t19-,20-,21-,22-,23-,24-/m1/s1
|
| Chemical Name |
(2R)-2-amino-N-[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide
|
| 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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~52.40 mM)
DMSO : ~5 mg/mL (~5.24 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (104.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0481 mL | 5.2403 mL | 10.4806 mL | |
| 5 mM | 0.2096 mL | 1.0481 mL | 2.0961 mL | |
| 10 mM | 0.1048 mL | 0.5240 mL | 1.0481 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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