SPACE peptide
目录号 : GC34274
SPACE肽是一种皮肤穿透肽，能够促进分子进入皮肤。
Cas No.:1621717-95-0
Sample solution is provided at 25 µL, 10mM.
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SPACE peptide is a skin penetrating peptide which facilitates the delivery of molecules through the skin.
SPACE peptide, when conjugates to cargoes such as small molecules and proteins, is able to facilitate their penetration across the stratum corneum into epidermis and dermis. The peptide also exhibits increased penetration into various cells including keratinocytes, fibroblasts, and endothelial cells, likely through a macropinocytosis pathway[1]. SPACE enhances cyclosporine A, penetration into the skin significantly. It does not alter the skin lipid barrier. It interacts with skin proteins and induces changes in skin protein secondary structures (α-helices, β-sheet, random coils and turns). SPACE enhances cyclosporine A skin penetration, via a transcellular pathway, enhancing its partitioning into keratin-rich corneocytes through concurrent binding of SPACE with keratin and cyclosporine A. Interaction between SPACE and keratin best correlates with measured cyclosporine A skin transport[2]. SPACE-peptide in combination with a DOTAP-based ethosomal carrier system can enhance skin delivery of siRNA[3]. The SPACE-ethosomal system enhances hyaluronic acid penetration into porcine skin in vitro by 7.8+/-1.1-fold compared to PBS[4].
The efficacy of DOTAP-SES in delivering GAPDH-siRNA into skin is confirmed in BALB/C mice. Topical application of DOTAP-SES on mice skin results in 63.2%±7.7% of GAPDH knockdown, which is significantly higher than that from GAPDH-siRNA PBS (p<0.05) [3].
[1]. 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. [2]. Kumar S, et al. Peptides as skin penetration enhancers: mechanisms of action. J Control Release. 2015 Feb 10;199:168-78. [3]. Chen M, et al. Topical delivery of siRNA into skin using SPACE-peptide carriers. J Control Release. 2014 Apr 10;179:33-41. [4]. Chen M, et al. Topical delivery of hyaluronic acid into skin using SPACE-peptide carriers. J Control Release. 2014 Jan 10;173:67-74.
Cell experiment: | The cytotoxicity of SPACE peptide is assessed using the MTT Cell Proliferation Assay. HEKa cells are seeded in 96-well microplates at a density of 5000 cells/well. Cultures are allowed to grow until they reaches ~80% confluency. Cells are then incubated with 150 μL of 10, 5, 2.5, or 1.25 mg/mL SPACE peptide in media. Media only is used as a negative control, and media without cells is used to subtract background. Cytotoxicity is assessed for 1, 4, and 12 h incubation periods[2]. |
Animal experiment: | Mice: Female BALB/c mice (knockdown of GAPDH protein) are anesthetized using isoflurane inhalation (2-3%), the back skin of animals is shaved, and a cylinder with an exposed skin area of 1.8 cm2 is attached to the back of mice. 200 μL of the SPACE peptide is topically applied in the attached cylinder, and is manually spread over the entire exposure area. Applied test solutions are allowed to incubate with the exposed skin for 6 hours while keeping animals under minimal anesthesia. After 6 hours, the cylinder is carefully removed, and the entire exposure area is covered with sterile gauze and a breathable bandage. After 72 hrs, animals are sacrificed and skin biopsies (5 mm diameter) are collected from treated area of the animal’s skin. Total protein concentration in the skin biopsy tissue is determined[3]. |
References: [1]. 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. | |
| Cas No. | 1621717-95-0 | SDF | |
| Canonical SMILES | Ala-Cys-Thr-Gly-Ser-Thr-Gln-His-Gln-Cys-Gly (Disulfide bridge: Cys2-Cys10) | ||
| 分子式 | C40H63N15O17S2 | 分子量 | 1090.17 |
| 溶解度 | DMSO : 100 mg/mL (91.73 mM);Water : 50 mg/mL (45.86 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9173 mL | 4.5864 mL | 9.1729 mL |
| 5 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL |
| 10 mM | 0.0917 mL | 0.4586 mL | 0.9173 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet