Disitertide (P144) TFA 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 TFA 也是PI3K的抑制剂和凋亡 (apoptosis) 诱导剂。
生物活性 | Disitertide (P144) TFA is a peptidictransforming growth factor-beta 1 (TGF-β1)inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also aPI3Kinhibitor and anapoptosisinducer[1][2][3][4][5].
|
IC50& Target | |
体外研究 (In Vitro) | Disitertide (P144, 100 μg/mL) TFA 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) TFA 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) TFA 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. |
|
体内研究 (In Vivo) | Disitertide (P144, Topical application, 300 μg/mL) TFA 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. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
Sequence Shortening | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture and light Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(29.50 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 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 |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (1.48 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (1.48 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (1.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (1.48 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|