| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target of the SPACE peptide is the lipid and protein matrix of the skin‘s stratum corneum barrier. It likely interacts with keratin and other skin proteins, inducing transient changes in the protein secondary structure (e.g., altering alpha-helices and beta-sheets) to enhance paracellular and transcellular transport of conjugated cargo molecules.
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| ln Vitro |
When conjugated to payloads like proteins and tiny molecules, SPACE peptide can help these molecules pass through the stratum corneum and enter the epidermis and dermis[2]. Additionally, SPACE peptide shows enhanced uptake by keratinocytes, fibroblasts, and endothelial cells[2], most likely via a macropinocytosis pathway. By concurrently associating SPACE with keratin and Cyclosporine A, SPACE peptide increases Cyclosporine A's skin penetration through a transcellular channel and improves its partitioning into keratin-rich corneocytes[3].
In vitro, SPACE peptide enhances the penetration of conjugated macromolecules such as hyaluronic acid (HA) through full-thickness porcine skin or human skin equivalents. It increases the transport of these large molecules by 7-8 fold compared to control. When conjugated to cyclosporine A, it facilitates drug partitioning into keratin-rich corneocytes via concurrent binding with keratin. |
| ln Vivo |
In vivo, topical application of SPACE peptide in a DOTAP-based ethosomal carrier system delivers siRNA into the skin of BALB/c mice. This results in significant gene knockdown (63.2% for GAPDH-siRNA) compared to siRNA in PBS, demonstrating its ability to facilitate the transdermal delivery of nucleic acids and other therapeutic macromolecules.
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| Enzyme Assay |
A direct non-cellular binding assay can be used to study the interaction with keratin. Purified keratin protein is immobilized on an ELISA plate. Biotinylated SPACE peptide is added at varying concentrations. Binding is detected with streptavidin-HRP and a colorimetric substrate. This assay is used to determine the binding affinity (Kd) and to confirm that the interaction with keratin correlates with enhanced skin transport.
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| Cell Assay |
The primary in vitro skin penetration assay uses a Franz diffusion cell system. A skin membrane (e.g., porcine ear skin or human cadaver skin) is mounted between the donor and receptor chambers. A fluorescently-labeled cargo (e.g., FITC-hyaluronic acid) conjugated to SPACE peptide is applied to the donor chamber. The receptor chamber is filled with PBS. At regular intervals (e.g., 6, 12, 24 h), samples are withdrawn and the fluorescence is measured to quantify the cumulative amount of cargo that has penetrated the skin.
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| Animal Protocol |
An in vivo animal protocol uses the BALB/c mouse model for siRNA delivery. A SPACE peptide-based ethosomal formulation containing siRNA against GAPDH (glyceraldehyde 3-phosphate dehydrogenase) is prepared. This formulation is applied topically to the shaved dorsal skin of mice for 6-8 hours. After treatment, skin biopsies are collected. The GAPDH mRNA and protein levels are measured by qRT-PCR and Western blot to assess the percentage of gene knockdown (e.g., 63.2% reported).
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| ADME/Pharmacokinetics |
As a peptide, SPACE is expected to have poor systemic absorption due to its hydrophilic nature and the barrier function of the skin. When applied topically, it remains largely localized in the stratum corneum and viable epidermis. Any peptide that enters the systemic circulation is rapidly degraded by proteases. Half-life in the blood is expected to be very short (minutes).
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| Toxicity/Toxicokinetics |
SPACE peptide is derived from naturally occurring amino acids and is considered to have low inherent toxicity. It does not alter the skin lipid barrier irreversibly. In vitro, it does not cause significant cell death at effective concentrations (e.g., < 1 mM). In mice, repeated topical application does not cause visible skin irritation, redness, or systemic distress at the doses used for gene knockdown studies.
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| References |
[1]. Chen M, et al. Topical delivery of hyaluronic acid into skin using SPACE-peptide carriers. J Control Release. 2014 Jan 10;173:67-74.
[2]. Hsu T, et al. Delivery of siRNA and other macromolecules into skin and cells using a peptide enhancer. Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15816-21. [3]. Kumar S, et al. Peptides as skin penetration enhancers: mechanisms of action. J Control Release. 2015 Feb 10;199:168-78 |
| Additional Infomation |
SPACE peptide is a 11-amino acid cyclic peptide with a disulfide bond between Cys(1) and Cys(10). Its name is derived from “Skin Penetrating and Cell Entering.” It can be conjugated to a wide range of payloads including proteins (e.g., hyaluronic acid), small molecules (e.g., cyclosporine A), and nucleic acids (siRNA). It is a research-grade product and is not FDA-approved.
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| Exact Mass |
1089.397
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|---|---|
| CAS # |
1621717-95-0
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| PubChem CID |
170907819
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
18
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
74
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| Complexity |
2060
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@H]([C@H]1C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](C)N)C(=O)NCC(=O)O)CCC(=O)N)CC2=CN=CN2)CCC(=O)N)[C@@H](C)O)CO)O
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| InChi Key |
NDGGTJRAQNJEBK-GTKCDMHESA-N
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| InChi Code |
InChI=1S/C40H63N15O17S2/c1-16(41)32(64)52-25-14-74-73-13-24(33(65)46-11-29(62)63)53-35(67)20(4-6-26(42)59)49-36(68)22(8-19-9-44-15-47-19)51-34(66)21(5-7-27(43)60)50-40(72)31(18(3)58)55-37(69)23(12-56)48-28(61)10-45-39(71)30(17(2)57)54-38(25)70/h9,15-18,20-25,30-31,56-58H,4-8,10-14,41H2,1-3H3,(H2,42,59)(H2,43,60)(H,44,47)(H,45,71)(H,46,65)(H,48,61)(H,49,68)(H,50,72)(H,51,66)(H,52,64)(H,53,67)(H,54,70)(H,55,69)(H,62,63)/t16-,17+,18+,20-,21-,22-,23-,24-,25-,30-,31-/m0/s1
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| Chemical Name |
2-[[(4R,7S,10S,13S,16S,19S,25S,28R)-7,13-bis(3-amino-3-oxopropyl)-28-[[(2S)-2-aminopropanoyl]amino]-16,25-bis[(1R)-1-hydroxyethyl]-19-(hydroxymethyl)-10-(1H-imidazol-5-ylmethyl)-6,9,12,15,18,21,24,27-octaoxo-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacosane-4-carbonyl]amino]acetic 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, 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) |
DMSO: 100 mg/mL (91.73 mM)
H2O: 50 mg/mL (45.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (91.73 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
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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