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| 10mg |
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| Targets |
Histatin-3 has multiple targets. It is a substrate for proprotein convertase 1 (PC1), an endoprotease. It also acts as a moderately potent, reversible, and competitive inhibitor of the proprotein convertases furin and PC7. Its antimicrobial mechanism involves binding to microbial membranes and disruption of cellular function.
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| ln Vitro |
Histatin-3 possesses powerful antimicrobial properties against a broad spectrum of fungi and bacteria. It has been shown to bind to microbial membranes. As a biochemical agent, it also has specific activity against human proteases: it inhibits furin-mediated cleavage with an estimated Ki of 1.98 uM and acts as a substrate for PC1.
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| ln Vivo |
Specific in vivo activity is not detailed in the provided sources. As a human salivary peptide, its physiological role is in maintaining oral health. Its effects on disease models would be the subject of active research, but it is not administered as a systemic therapeutic agent.
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| Enzyme Assay |
A common non-cellular assay is a protease inhibition assay. For this, a fluorogenic substrate (e.g., pGlu-Arg-Thr-Lys-Arg-MCA) is incubated with a purified furin enzyme in a suitable buffer. Various concentrations of Histatin-3 are added to the reaction mixture. The enzymatic cleavage of the substrate releases a fluorescent molecule (MCA). The increase in fluorescence over time is measured using a plate reader to determine the inhibition constant (Ki).
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| Cell Assay |
To assess Histatin-3's effect on cells, an antimicrobial susceptibility assay is used. A standardized suspension of a target microorganism (e.g., Candida albicans) is prepared. Serial two-fold dilutions of Histatin-3 are mixed with the microbial suspension in a 96-well plate. After an incubation period (e.g., 2 hours for fungi), the plates are plated onto agar or the metabolic activity of the organisms is measured (e.g., with XTT assay). The Minimum Fungicidal Concentration (MFC) or IC₅0 can then be determined.
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| Animal Protocol |
Specific protocols for in vivo animal studies are not provided. For a peptide like Histatin-3, animal studies are often performed to evaluate its potential in oral diseases. A typical model might be a rodent model of oral candidiasis (thrush). The animals' mouths are swabbed with a cotton tip containing a suspension of C. albicans to establish an infection. Following infection, Histatin-3 solution is applied topically to the oral cavity multiple times per day. The therapeutic effect is then assessed by measuring the fungal burden (colony-forming units) on the tongue or buccal mucosa.
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| ADME/Pharmacokinetics |
As a naturally occurring peptide, its pharmacokinetics (PK) are part of its physiological role. When administered as a therapeutic, however, peptides generally have poor oral bioavailability and are rapidly degraded by proteases in the gastrointestinal tract and serum. Its half-life in circulation is expected to be very short. These factors present significant challenges for systemic drug development.
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| Toxicity/Toxicokinetics |
As a naturally occurring human peptide, it is non-toxic to human cells at its normal physiological concentrations. Its safety profile is inherent to its role in saliva. No significant systemic toxicity from Histatin-3 is reported in the provided documents, and it is generally regarded as safe.
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| References |
[1]. A Basak, et al. Histidine-rich human salivary peptides are inhibitors of proprotein convertases furin and PC7 but act as substrates for PC1. J Pept Res. 1997 Jun;49(6):596-603.
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| Additional Infomation |
Histatin-3 is an endogenous peptide of the innate immune system. Its dual role as a protease substrate and inhibitor is notable; it acts as a natural regulator of proprotein convertases. While it is a promising lead for antimicrobial drug development, particularly for oral or topical applications, it is not an FDA-approved drug. The search results provide its precise amino acid sequence, confirming its identity as a human salivary peptide.
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| Molecular Formula |
C178H258N64O48
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| Molecular Weight |
4062.35
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| CAS # |
112844-49-2
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| PubChem CID |
91668153
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
68
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| Hydrogen Bond Acceptor Count |
64
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| Rotatable Bond Count |
139
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| Heavy Atom Count |
290
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| Complexity |
9630
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| Defined Atom Stereocenter Count |
30
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (12.31 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2462 mL | 1.2308 mL | 2.4616 mL | |
| 5 mM | 0.0492 mL | 0.2462 mL | 0.4923 mL | |
| 10 mM | 0.0246 mL | 0.1231 mL | 0.2462 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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