| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
The primary target for KALA is the liposomal or cellular membrane. By forming an alpha-helical structure, it inserts into and destabilizes the lipid bilayer, facilitating membrane fusion. For liver targeting, it achieves effective transfection by binding to asialoglycoprotein/galactose receptors on hepatocytes.
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| ln Vitro |
Bone marrow-derived dendritic cells (BMDCs) exhibit enhanced transgene expression and immunological activation upon modification of a plasmid DNA-encapsulating liposomal membrane with the KALA peptide[1].
In vitro, KALA modifies the liposomal membrane encapsulating plasmid DNA, leading to enhanced transgene expression and immune activation. When used to coat DNA-loaded nanoparticles, it promotes cellular uptake and endosomal escape. In bone marrow-derived dendritic cells (BMDCs), KALA-functionalized liposomes significantly enhance gene delivery efficiency compared to unmodified liposomes. |
| ln Vivo |
Specific in vivo activity data for KALA is tied to its function as a delivery vehicle. When administered intravenously (e.g., in a liposomal formulation), the KALA peptide facilitates the accumulation and transfection of the payload in the liver. This leads to successful expression of the delivered gene (e.g., a reporter gene like luciferase) in hepatic tissue, demonstrating targeted gene delivery.
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| Enzyme Assay |
KALA itself is not an active pharmaceutical ingredient requiring a functional assay. However, its membrane fusogenic activity can be measured in a non-cellular lipid mixing assay. Liposomes containing a self-quenching concentration of a fluorescent lipid (e.g., R18) are prepared. Mixing these liposomes with KALA in buffer leads to membrane fusion, resulting in lipid dilution and a measurable increase in fluorescence intensity.
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| Cell Assay |
The primary in vitro cellular assay for KALA involves gene delivery. A plasmid DNA encoding a reporter gene (e.g., GFP or luciferase) is complexed with a cationic liposome formulation that includes KALA. Cultured cells (e.g., HepG2 liver cancer cells) are incubated with the DNA-liposome-KALA complexes for 4-6 hours. After 24-48 hours, transfection efficiency is quantified by measuring the reporter gene signal (e.g., fluorescence or luminescence) and compared to controls without KALA.
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| Animal Protocol |
For in vivo evaluation, a mouse model is used. Plasmid DNA (e.g., encoding luciferase) is formulated with a liposome and KALA. The complexes are injected intravenously (via tail vein) into mice. After 24-48 hours, the mice are sacrificed and organs (liver, spleen, lung) are harvested. Luciferase activity is measured using a luminometer after adding the substrate, and results are expressed as relative light units (RLU) per mg of tissue protein to determine the efficiency of liver-targeted gene delivery.
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| ADME/Pharmacokinetics |
As a peptide, KALA‘s PK is not studied as a drug candidate. Instead, its stability in serum is assessed. The peptide is incubated in 50% mouse serum at 37degC, and its degradation is monitored by HPLC at various time points. KALA is expected to be rapidly cleaved by proteases, with a half-life likely less than 1-2 hours in circulation.
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| Toxicity/Toxicokinetics |
KALA is used as a research reagent and is not intended for therapeutic use, so clinical toxicity studies are not available. As a cationic membrane-active peptide, the primary toxicity is physical disruption of cell membranes at high concentrations. In vitro, at concentrations above 50 ug/mL, it may cause significant cell lysis. In vivo, its degradation products are non-toxic amino acids.
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| References |
[1]. Naoya Miura, et al. Identification and Evaluation of the Minimum Unit of a KALA Peptide Required for Gene Delivery and Immune Activation. J Pharm Sci. 2017 Oct;106(10):3113-3119.
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| Additional Infomation |
KALA consists of 30 amino acids (WEAKLAKALAKALAKHLAKALAKALKACEA) with a molecular weight of 3131.82. Its name is derived from a combination of amino acids that form the helical structure. It is a versatile tool for enhancing the intracellular delivery of nucleic acids, peptides, and small molecules. It is not approved for clinical gene therapy.
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| Molecular Formula |
C144H248N40O35S
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|---|---|
| Molecular Weight |
3131.82
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| Exact Mass |
3129.857
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| CAS # |
187987-64-0
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
2669.2±65.0 °C at 760 mmHg
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| Flash Point |
1568.1±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
-1.26
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| SMILES |
SC[C@@H](C(N[C@H](C(N[C@H](C(=O)O)C)=O)CCC(=O)O)=O)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](CC1=CNC=N1)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](CCCCN)NC([C@H](C)NC([C@H](CCC(=O)O)NC([C@H](CC1=CNC2C=CC=CC1=2)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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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) |
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
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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 | 0.3193 mL | 1.5965 mL | 3.1930 mL | |
| 5 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | |
| 10 mM | 0.0319 mL | 0.1597 mL | 0.3193 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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