| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
The primary target is the cell membrane, where the positively charged RALA peptide interacts with negatively charged membrane phospholipids. It has pH-responsive binding properties that enhance alpha-helical membrane insertion, allowing it to deliver genetic material into the cytoplasm. It also targets bone and cancer cells for therapeutic delivery.
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| ln Vitro |
In vitro, RALA peptide forms stable nanocomplexes with plasmid DNA and siRNA, protecting nucleic acids from nuclease degradation. It enhances gene transfection efficiency in a variety of cell lines, including prostate cancer and breast cancer cells. It also promotes the delivery of bisphosphonates, enhancing their anti-cancer activity, and promotes osteoblast collagen deposition and extracellular matrix mineralization in bone tissue engineering applications.
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| ln Vivo |
In vivo, RALA peptide (as a non-viral vector) enhances the delivery of therapeutic nucleic acids to target tissues. It has been used to deliver bisphosphonates for improved anti-tumor activity in prostate and breast cancer models. Due to its high transfection efficiency and low immunogenicity compared to viral vectors, it is a promising tool for gene therapy and regenerative medicine.
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| Enzyme Assay |
RALA peptide's ability to bind DNA is measured using a gel retardation assay. Varying weight/charge ratios of RALA peptide are mixed with a fixed amount of plasmid DNA. The complexes are loaded onto an agarose gel with a DNA intercalating dye. Complete migration of DNA into the gel indicates insufficient binding; retention of DNA in the well indicates stable complex formation. The ratio where mobility is fully retarded indicates optimal complexation.
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| Cell Assay |
Transfection efficiency is measured using a reporter gene assay. Cells (e.g., HEK293 or HeLa) are seeded in 24-well plates (5×10⁴ cells/well). RALA peptide is complexed with plasmid DNA encoding GFP or luciferase at optimized ratios and incubated for 20-30 minutes. The complexes are added to cells and incubated for 4-6 hours. After 48 hours, GFP expression is quantified by flow cytometry, or luciferase activity is measured using a luminometer after adding the substrate. Cytotoxicity is assessed by MTT assay.
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| Animal Protocol |
An in vivo gene delivery protocol is used in tumor-bearing mice. Nude mice are implanted subcutaneously with a tumor cell line (e.g., prostate cancer). RALA peptide complexed with a therapeutic plasmid (e.g., encoding a tumor suppressor or pro-apoptotic gene) is administered intratumorally (i.t.) or intravenously (i.v.) at a dose of 10-50 microg of DNA per mouse. After 48-72 hours, tumors are harvested, sectioned, and examined for transgene expression by immunohistochemistry or fluorescence microscopy. Tumor growth is monitored over 2-3 weeks.
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| ADME/Pharmacokinetics |
RALA peptide has a molecular weight of 3327.92 (C144H248N54O35S). Its sequence is WEARLARALARALARHLARALARALRACEA. It is soluble in DMSO (50 mg/mL with pH adjustment using 1 M HCl) and is stored as a solid at -20degC. Pharmacokinetic properties are not extensively characterized, but as a peptide, it is rapidly degraded by proteases in circulation, necessitating local administration for optimal delivery.
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| Toxicity/Toxicokinetics |
RALA peptide shows low cytotoxicity in vitro at concentrations used for gene delivery (typically 1-50 microg/mL). It is considered safe for research applications. In vivo, no significant systemic toxicity has been reported following intratumoral or local injection at effective doses. Standard laboratory precautions (gloves, eye protection) are recommended for handling. It is not intended for human use.
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| References |
[1]. Liu Y, et, al. Development and Characterization of High Efficacy Cell-Penetrating Peptide via Modulation of the Histidine and Arginine Ratio for Gene Therapy. Materials (Basel). 2021 Aug 19;14(16):4674.
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| Additional Infomation |
RALA peptide is derived from a 30-residue arginine-rich sequence and was developed as a non-toxic alternative to viral vectors. Its pH-responsive alpha-helical conformation enhances endosomal escape and transfection efficiency. It is primarily a research-grade product for laboratory applications in gene therapy, cancer research, and tissue engineering. It has not been approved for clinical gene therapy.
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| Exact Mass |
3326.904
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|---|---|
| CAS # |
1613231-49-4
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| PubChem CID |
171042932
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
57
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| Hydrogen Bond Acceptor Count |
45
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| Rotatable Bond Count |
117
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| Heavy Atom Count |
234
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| Complexity |
7760
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| Defined Atom Stereocenter Count |
30
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)N
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| InChi Key |
GHWPWGCKSQQQSL-VKNOPYHSSA-N
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| InChi Code |
InChI=1S/C144H248N54O35S/c1-66(2)54-98(191-114(209)78(19)171-121(216)90(37-28-48-162-139(148)149)184-111(206)75(16)179-132(227)101(57-69(7)8)195-127(222)94(41-32-52-166-143(156)157)186-108(203)72(13)175-125(220)96(43-45-106(199)200)188-119(214)87(145)60-84-62-168-88-35-26-25-34-86(84)88)129(224)176-73(14)109(204)182-89(36-27-47-161-138(146)147)120(215)170-80(21)116(211)193-100(56-68(5)6)131(226)178-77(18)113(208)187-95(42-33-53-167-144(158)159)128(223)197-104(61-85-63-160-65-169-85)135(230)196-102(58-70(9)10)133(228)180-76(17)112(207)185-91(38-29-49-163-140(150)151)122(217)172-79(20)115(210)192-99(55-67(3)4)130(225)177-74(15)110(205)183-92(39-30-50-164-141(152)153)123(218)173-81(22)117(212)194-103(59-71(11)12)134(229)189-93(40-31-51-165-142(154)155)124(219)174-82(23)118(213)198-105(64-234)136(231)190-97(44-46-107(201)202)126(221)181-83(24)137(232)233/h25-26,34-35,62-63,65-83,87,89-105,168,234H,27-33,36-61,64,145H2,1-24H3,(H,160,169)(H,170,215)(H,171,216)(H,172,217)(H,173,218)(H,174,219)(H,175,220)(H,176,224)(H,177,225)(H,178,226)(H,179,227)(H,180,228)(H,181,221)(H,182,204)(H,183,205)(H,184,206)(H,185,207)(H,186,203)(H,187,208)(H,188,214)(H,189,229)(H,190,231)(H,191,209)(H,192,210)(H,193,211)(H,194,212)(H,195,222)(H,196,230)(H,197,223)(H,198,213)(H,199,200)(H,201,202)(H,232,233)(H4,146,147,161)(H4,148,149,162)(H4,150,151,163)(H4,152,153,164)(H4,154,155,165)(H4,156,157,166)(H4,158,159,167)/t72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,87-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-5-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(2R)-1-[[(2S)-4-carboxy-1-[[(1S)-1-carboxyethyl]amino]-1-oxobutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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) |
DMSO: 50 mg/mL (15.02 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.) |
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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