Transdermal Peptide (TD 1 (peptide))
(Synonyms: 透皮短肽) 目录号 : GC30535
Transdermal Peptide（TD 1（肽））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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
|
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 [2]: | |
|
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 [3]: | |
|
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. |
|
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.
透皮肽（TD 1（肽））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].
| 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。 |
||
| 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 | |||
 |
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。
Phase III Study of Adjuvant Ipilimumab (3 or 10 mg/kg) Versus High-Dose Interferon Alfa-2b for Resected High-Risk Melanoma: North American Intergroup E1609
J Clin Oncol2020 Feb 20;38(6):567-575.PMID: 31880964DOI: 10.1200/JCO.19.01381
Purpose: Phase III adjuvant trials have reported significant benefits in both relapse-free survival (RFS) and overall survival (OS) for high-dose interferon alfa (HDI) and ipilimumab at 10 mg/kg (ipi10). E1609 evaluated the safety and efficacy of ipilimumab at 3 mg/kg (ipi3) and ipi10 versus HDI. Patients and methods: E1609 was a phase III trial in patients with resected cutaneous melanoma (American Joint Committee on Cancer 7th edition stage IIIB, IIIC, M1a, or M1b). It had 2 coprimary end points: OS and RFS. A 2-step hierarchic approach first evaluated ipi3 versus HDI followed by ipi10 versus HDI. Results: Between May 2011 and August 2014, 1,670 adult patients were centrally randomly assigned (1:1:1) to ipi3 (n = 523), HDI (n = 636), or ipi10 (n = 511). Treatment-related adverse events grade ¡ݠ3 occurred in 37% of patients receiving ipi3, 79% receiving HDI, and 58% receiving ipi10, with adverse events leading to treatment discontinuation in 35%, 20%, and 54%, respectively. Comparison of ipi3 versus HDI used an intent-to-treat analysis of concurrently randomly assigned patient cases (n = 1,051) and showed significant OS difference in favor of ipi3 (hazard ratio [HR], 0.78; 95.6% repeated CI, 0.61 to 0.99; P = .044; RFS: HR, 0.85; 99.4% CI, 0.66 to 1.09; P = .065). In the second step, for ipi10 versus HDI (n = 989), trends in favor of ipi10 did not achieve statistical significance. Salvage patterns after melanoma relapse showed significantly higher rates of ipilimumab and ipilimumab/anti-programmed death 1 use in the HDI arm versus ipi3 and ipi10 (P ¡ܠ.001). Conclusion: Adjuvant therapy with ipi3 benefits survival versus HDI; for the first time to our knowledge in melanoma adjuvant therapy, E1609 has demonstrated a significant improvement in OS against an active control regimen. The currently approved adjuvant ipilimumab dose (ipi10) was more toxic and not superior in efficacy to HDI.
Glucose-Responsive Microneedle Patches for Diabetes Treatment
J Diabetes Sci Technol2019 Jan;13(1):41-48.PMID: 29848105DOI: 10.1177/1932296818778607
Antidiabetic therapeutics, including insulin as well as glucagon-like peptide 1 (GLP-1) and its analogs, are essential for people with diabetes to regulate their blood glucose levels. Nevertheless, conventional treatments based on hypodermic administration is commonly associated with poor blood glucose control, a lack of patient compliance, and a high risk of hypoglycemia. Closed-loop drug delivery strategies, also known as self-regulated administration, which can intelligently govern the drug release kinetics in response to the fluctuation in blood glucose levels, show tremendous promise in diabetes therapy. In the meantime, the advances in the development and use of microneedle (MN)-array patches for transdermal drug delivery offer an alternative method to conventional hypodermic administration. Hence, glucose-responsive MN-array patches for the treatment of diabetes have attracted increasing attentions in recent years. This review summarizes recent advances in glucose-responsive MN-array patch systems. Their opportunities and challenges for clinical translation are also discussed.
Microneedle Mediated Transdermal Delivery of Protein, Peptide and Antibody Based Therapeutics: Current Status and Future Considerations
Pharm Res2020 Jun 2;37(6):117.PMID: 32488611DOI: 10.1007/s11095-020-02844-6
The success of protein, peptide and antibody based therapies is evident - the biopharmaceuticals market is predicted to reach $388 billion by 2024 [1], and more than half of the current top 20 blockbuster drugs are biopharmaceuticals. However, the intrinsic properties of biopharmaceuticals has restricted the routes available for successful drug delivery. While providing 100% bioavailability, the intravenous route is often associated with pain and needle phobia from a patient perspective, which may translate as a reluctance to receive necessary treatment. Several non-invasive strategies have since emerged to overcome these limitations. One such strategy involves the use of microneedles (MNs), which are able to painlessly penetrate the stratum corneum barrier to dramatically increase transdermal drug delivery of numerous drugs. This review reports the wealth of studies that aim to enhance transdermal delivery of biopharmaceutics using MNs. The true potential of MNs as a drug delivery device for biopharmaceuticals will not only rely on acceptance from prescribers, patients and the regulatory authorities, but the ability to upscale MN manufacture in a cost-effective manner and the long term safety of MN application. Thus, the current barriers to clinical translation of MNs, and how these barriers may be overcome are also discussed.
Patch Pumps for Insulin
J Diabetes Sci Technol2019 Jan;13(1):27-33.PMID: 30070604DOI: 10.1177/1932296818786513
Newly developed patch pumps are starting to occupy a noticeable fraction of the insulin delivery market. New entrants, using novel technologies, promise accurate, flexible insulin delivery at lower costs. In the section, we review the currently available devices, discuss some of the devices on the horizon, and speculate about some fascinating new approaches. In this first article, we provide an overview of the simplified devices-V-Go, PAQ, and One Touch Via-and of the more complex devices-Omnipod, Cellnovo, JewelPump, Solo, SFC Fluidics pump, Libertas, Medtronic pump, and EOPatch. We also discuss controllers, smartphones, and cybersecurity.
Peptide-mediated transdermal delivery of botulinum neurotoxin type A reduces neurogenic inflammation in the skin
Pain2010 May;149(2):316-324.PMID: 20223589DOI: 10.1016/j.pain.2010.02.024
Release of inflammatory pain mediators from peripheral sensory afferent endings contributes to the development of a positive feedback cycle resulting in chronic inflammation and pain. Botulinum neurotoxin type A (BoNT-A) blocks exocytosis of neurotransmitters and may therefore block the release of pain modulators in the periphery. Subcutaneous administration of BoNT-A (2.5, 5 and 10U) reduced plasma extravasation (PE) caused by electrical stimulation of the saphenous nerve or capsaicin in the rat hindpaw skin (ANOVA, Post hoc Tukey, p<0.05, n=6). Subcutaneous BoNT-A also reduced blood flow changes evoked by saphenous nerve stimulation (ANOVA, Post hoc Tukey, p<0.05, n=6). Subcutaneous BoNT-A had no effect on PE induced by local injection of substance P (SP) or vasodilation induced by local CGRP injection. Although BoNT-A is an effective treatment for a wide range of painful conditions, the toxin's large size necessitates that it be injected at numerous sites. We found that a short synthetic peptide (TD-1) can facilitate effective transdermal delivery of BoNT-A through intact skin. Coadministration of TD-1 and BoNT-A to the hindpaw skin resulted in a significant reduction in PE evoked by electrical stimulation. The findings show that BoNT-A can be administered subcutaneously or topically with a novel transdermal delivery peptide to reduce inflammation produced by activating nociceptors in the skin. Peptide-mediated delivery of BoNT-A is an easy and non-invasive way of administering the toxin that may prove to be useful in clinical practice.