Transdermal Peptide (TD 1 (peptide))
(Synonyms: 透皮短肽) 目录号 : GC30535
Transdermal Peptide (TD 1 (peptide)) 由 11 个氨基酸组成，是第一个通过噬菌体展示发现的透皮增强肽。
Cas No.:918629-48-8
Sample solution is provided at 25 µL, 10mM.
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Transdermal Peptide (TD 1 (peptide)), consisting of 11 amino acids, is the first transdermal enhancing peptide discovered by phage display. Transdermal Peptide binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules[1,2]. Transdermal Peptide (TD 1 (peptide))1 has been found to facilitate the transdermal delivery of many macromolecules such as botulinum neurotoxin type A (BoNT-A), growth hormone (GH), siRNA and human epidermal growth factor (hEGF) [3,4]. Energy is required for the Transdermal Peptide (TD 1 (peptide))-mediated transdermal protein delivery through rat and human skins.A novel energy-dependent permeation process during the Transdermal Peptide (TD 1 (peptide))-mediated transdermal protein delivery[7].
When ouabain was coadministered, the transdermal delivery of Transdermal Peptide (TD 1 (peptide))-hEGF, a fusion protein composed of Transdermal Peptide (TD 1 (peptide)) and hEGF, was significantly reduced. The addition of the exogenous competitor can also cause a decrease in the transdermal delivery of Transdermal Peptide (TD 1 (peptide))-hEGF. Therefore, ATP1B1 played a key role in the peptide-directed drug delivery across the skin[1].
Coadministration of Transdermal Peptide (TD 1 (peptide)) and insulin to the abdominal skin of diabetic rats resulted in elevated systemic levels of insulin and suppressed serum glucose levels for at least 11 h. Significant systemic bioavailability of human growth hormone was also achieved when topically coadministered with Transdermal Peptide (TD 1 (peptide)) [2]. Blood glucose level lowered to about 26% of initial after administrating 2.1 IU insulin with 0.5 µmol of TD-34 in 100 µL of saline for 8 h to diabetic rats in vivo[6]. Transdermal Peptide (TD 1 (peptide)) delivery of anti-GAPDH siRNA significantly reduced the level of GAPDH in 72 h. Transdermal Peptide (TD 1 (peptide)) can create a transient opening in non-follicle rat skin for delivery of siRNA and reveal a novel mechanism of transdermal delivery of Transdermal Peptide (TD 1 (peptide)) and siRNA into the epidermis for gene knockdown[5].
References:
[1]: Wang C, Ruan R, et,al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67. doi: 10.1021/mp500789h. Epub 2015 Mar 23. PMID: 25734358.
[2]: Chen Y, Shen Y, et,al. Transdermal protein delivery by a coadministered peptide identified via phage display. Nat Biotechnol. 2006 Apr;24(4):455-60. doi: 10.1038/nbt1193. Epub 2006 Mar 26. PMID: 16565728.
[3]: Carmichael NME, Dostrovsky JO, et,al. Peptide-mediated transdermal delivery of botulinum neurotoxin type A reduces neurogenic inflammation in the skin. Pain. 2010 May;149(2):316-324. doi: 10.1016/j.pain.2010.02.024. Epub 2010 Mar 23. PMID: 20223589.
[4]: Zhang T, Qu H, et,al. Transmembrane delivery and biological effect of human growth hormone via a phage displayed peptide in vivo and in vitro. J Pharm Sci. 2010 Dec;99(12):4880-91. doi: 10.1002/jps.22203. PMID: 20821386.
[5]: Lin CM, Huang K, et,al. A simple, noninvasive and efficient method for transdermal delivery of siRNA. Arch Dermatol Res. 2012 Mar;304(2):139-44. doi: 10.1007/s00403-011-1181-5. Epub 2011 Oct 19. PMID: 22009459.
[6]: Chang M, Li X, et,al. Effect of cationic cyclopeptides on transdermal and transmembrane delivery of insulin. Mol Pharm. 2013 Mar 4;10(3):951-7. doi: 10.1021/mp300667p. Epub 2013 Feb 21. PMID: 23391375.
[7]: Ruan R, Jin P, et,al. Peptide-chaperone-directed transdermal protein delivery requires energy. Mol Pharm. 2014 Nov 3;11(11):4015-22. doi: 10.1021/mp500277g. Epub 2014 Oct 13. PMID: 25269793.
Transdermal Peptide (TD 1 (peptide)) 由 11 个氨基酸组成，是第一个通过噬菌体展示发现的透皮增强肽。透皮肽与 Na+/K+-ATPase β-亚基 (ATP1B1) 结合，增强许多大分子的透皮递送[1,2]。透皮肽（TD 1（肽））1 已被发现可促进许多大分子的透皮递送，例如 A 型肉毒杆菌神经毒素 (BoNT-A)、生长激素 (GH)、siRNA 和人表皮生长因子 (hEGF) [3 ,4].透皮肽（TD 1（肽））介导的透皮蛋白质通过大鼠和人体皮肤递送需要能量。透皮肽（TD 1（肽））介导的透皮蛋白质递送过程中一种新型的能量依赖性渗透过程[7 .
当同时给予哇巴因时，透皮肽（TD 1（肽））-hEGF（一种由透皮肽（TD 1（肽））和 hEGF 组成的融合蛋白）的透皮递送显着降低.添加外源性竞争剂也会导致透皮肽 (TD 1 (肽))-hEGF 的透皮递送减少。因此，ATP1B1 在通过皮肤的肽导向药物递送中发挥了关键作用[1]。
透皮肽（TD 1（肽））和胰岛素共同给药至糖尿病大鼠的腹部皮肤导致全身胰岛素水平升高并抑制血清葡萄糖水平至少 11 小时。与透皮肽（TD 1（肽））[2] 局部联合给药时，人生长激素的全身生物利用度也显着提高。给予糖尿病大鼠体内 0.5 µmol TD-34 在 100 µL 生理盐水中 2.1 IU 胰岛素 8 小时后，血糖水平降至初始值的 26% 左右[6]。抗 GAPDH siRNA 的透皮肽（TD 1（肽））递送在 72 小时内显着降低了 GAPDH 的水平。透皮肽（TD 1（肽））可以在非毛囊大鼠皮肤中产生一个瞬时开口，用于递送 siRNA，并揭示一种将透皮肽（TD 1（肽））和 siRNA 经皮递送到表皮中以进行基因敲除的新机制[5].
| Kinase experiment [1]: | |
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Preparation Method |
Transdermal Peptide (TD 1 (peptide)) or ATP1B1 were incubated in 96-well plates with 0.05 M NaHCO 3 for 12 h at 4 °C. Cell lysates were incubated with fixed Transdermal Peptide (TD 1 (peptide)) for 2 h at 37°C. |
|
Reaction Conditions |
0.5 mg/mL Transdermal Peptide (TD 1 (peptide)) for 2 h at 37°C. |
|
Applications |
The interaction between Transdermal Peptide (TD 1 (peptide)) (0.5 mg/mL) and the full-length ATP1B1 or the C-terminus of ATP1B1 was dose-dependent. |
| Cell experiment [1]: | |
|
Cell lines |
HaCaT cells |
|
Preparation Method |
HaCaT cells were treated with Transdermal Peptide (TD 1 (peptide)) to study the expression of ATP1B1. |
|
Reaction Conditions |
20 μg/mL Transdermal Peptide (TD 1 (peptide)) |
|
Applications |
Transdermal Peptide (TD 1 (peptide)) affects the localization of ATP1B1 in HaCaT cells, ATP1B1 is initially uniformly distributed in cells, whereas after treatment with Transdermal Peptide (TD 1 (peptide)), it accumulates near the cell membrane. |
| Animal experiment [1]: | |
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Animal models |
Adult male SD rats (200 ± 10 g) |
|
Preparation Method |
For in vivo skin permeation, 50 μg of Transdermal Peptide (TD 1 (peptide))-hEGF was coadministered with 500 μg of ouabain, 50 μg of GST-ATP1B1, or 50 μg of GST (control group) on the abdomen of rats for 6 h. |
|
Dosage form |
50 μg Transdermal Peptide (TD 1 (peptide)) for 6h(i.p). |
|
Applications |
When ouabain was coadministered, the transdermal delivery of Transdermal Peptide (TD 1 (peptide))-hEGF, a fusion protein composed of Transdermal Peptide (TD 1 (peptide)) and hEGF, was significantly reduced. The addition of the exogenous competitor can also cause a decrease in the transdermal delivery of Transdermal Peptide (TD 1 (peptide))-hEGF. Therefore, ATP1B1 played a key role in the peptide-directed drug delivery across the skin. |
|
References: [1].Wang C, Ruan R,et,al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67. doi: 10.1021/mp500789h. Epub 2015 Mar 23. PMID: 25734358. |
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| Cas No. | 918629-48-8 | SDF | |
| 别名 | 透皮短肽 | ||
| Canonical SMILES | Ala-Cys-Ser-Ser-Ser-Pro-Ser-Lys-His-Cys-Gly | ||
| 分子式 | C40H66N14O16S2 | 分子量 | 1063.17 |
| 溶解度 | Soluble in Water | 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 | 0.9406 mL | 4.7029 mL | 9.4058 mL |
| 5 mM | 0.1881 mL | 0.9406 mL | 1.8812 mL |
| 10 mM | 0.0941 mL | 0.4703 mL | 0.9406 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
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- Purity: >98.00%
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