规格 | 价格 | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
靶点 |
TGF-β1, P13K[1][2].
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体外研究 (In Vitro) |
在 MC3T3-E1 细胞中,disitertide(P144,100 μg/mL)TFA 增加 Bax 蛋白的产生,同时抑制 PI3K 和 p-Akt [2]。 TFA 是 TGFβ1 的抑制剂,可抑制 GC 细胞中 MACC1-AS1 的表达,这表明预防 MSC 诱导的干细胞性和化疗耐药的可能策略是靶向 TGFβ 信号通路 [3]。 Disitertide(10 μg/mL 至 200 μg/mL)TFA 影响 GBM 细胞系 A172 和 U-87 MG 的生长、引发细胞凋亡并导致失巢凋亡 [5]。
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体内研究 (In Vivo) |
在裸鼠“体内”模型中治疗两周后,Dissolvertide(P144,局部给药,300 μg/mL)TFA 可改善肥厚性疤痕的形态并加速疤痕成熟 [4]。
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细胞实验 |
蛋白质印迹分析[2]
细胞类型: 小鼠胚胎成骨细胞前体 MC3T3-E1 细胞。 测试浓度:100 μg/mL。 孵化持续时间:4小时。 实验结果:与miR-590组相比,显着抑制MC3T3-E1细胞中PI3K和p-Akt蛋白表达水平,并诱导Bax蛋白表达。 |
动物实验 |
Animal/Disease Models: Human hypertrophic scars were implanted in 60 nude mice[4].
Doses: 300 μg/mL was added the Lipogel. Route of Administration: Topical application daily administered. Experimental Results: Successful shedding was achieved in 83,3% of the xenografts. |
参考文献 |
[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. |
分子式 |
C70H110N17O24S2F3
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分子量 |
1694.84
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相关CAS号 |
Disitertide diammonium;Disitertide;272105-42-7
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溶解度 (体外) |
H2O :< 0.1 mg/mL
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溶解度 (体内) |
Solubility in Formulation 1: 2.5 mg/mL (1.48 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (1.48 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (1.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 0.5900 mL | 2.9501 mL | 5.9003 mL | |
5 mM | 0.1180 mL | 0.5900 mL | 1.1801 mL | |
10 mM | 0.0590 mL | 0.2950 mL | 0.5900 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。