Disitertide diammonium
(Synonyms: P144 diammonium) 目录号 : GC68333Disitertide (P144) diammonium 是转化生长因子 TGFβ1 的多肽抑制剂，特异性的阻断其与受体间的相互作用。Disitertide diammonium 也是PI3K 的抑制剂和凋亡 (Apoptosis) 诱导剂。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an Apoptosis inducer[1][2][3][4][5].
Disitertide (P144, 100 μg/mL) diammonium suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells[2].
Disitertide (TGF-β1 inhibitor) diammonium abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance[3].
Disitertide (10 μg/mL to 200 μg/mL) diammonium affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines[5].
Western Blot Analysis[2]
| Cell Line: | Mouse embryo osteoblast precursor MC3T3-E1 cells. |
| Concentration: | 100 μg/mL |
| Incubation Time: | 4 h |
| Result: | Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group. |
Disitertide (P144, Topical application, 300 μg/mL) diammonium may promote scar maturation and improvement of hypertrophic scar morphology features in an "in vivo" model in nude mice after two weeks of treatment[4].
| Animal Model: | Human hypertrophic scars were implanted in 60 nude mice[4]. |
| Dosage: | 300 μg/mL was added the Lipogel. |
| Administration: | Topical application daily administered. |
| Result: | Successful shedding was achieved in 83.3% of the xenografts. |
[1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
[2]. Jun Yang, et al. Upregulation of microRNA-590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor-β1/phosphoinositide 3-kinase/Akt signaling. Int J Mol Med. 2019 May;43(5):2212-2220.
[3]. Wanming He, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654.
[4]. Shan Shan Qiu, et al. Effect of P144® (Anti-TGF-β) in an "In Vivo" Human Hypertrophic Scar Model in Nude Mice. PLoS One. 2015 Dec 31;10(12):e0144489.
[5]. Gabriel Gallo-Oller, et al. P144, a Transforming Growth Factor beta inhibitor peptide, generates antitumoral effects and modifies SMAD7 and SKI levels in human glioblastoma cell lines. Cancer Lett. 2016 Oct 10;381(1):67-75.
| Cas No. | SDF | Download SDF | |
| 别名 | P144 diammonium | ||
| 分子式 | C68H115N19O22S2 | 分子量 | 1614.88 |
| 溶解度 | DMSO : 10 mg/mL (6.19 mM; Need ultrasonic) | 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 | 0.6192 mL | 3.0962 mL | 6.1924 mL |
| 5 mM | 0.1238 mL | 0.6192 mL | 1.2385 mL |
| 10 mM | 0.0619 mL | 0.3096 mL | 0.6192 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。