Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Treprostinil Sodium (UT-15) 是有效的 DP1、IP 和 EP2 激动剂,EC50分别为0.6、1.9 和 6.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 455 | 待询 | ||
5 mg | ¥ 913 | 待询 | ||
10 mg | ¥ 1,460 | 待询 | ||
25 mg | ¥ 2,920 | 待询 | ||
50 mg | ¥ 4,680 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 983 | 现货 |
Treprostinil Sodium 的其他形式现货产品:
产品描述 | Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM). |
靶点活性 | RET:13 nM (Cell-free), VEGFR2:1 nM (Cell-free) |
体外活性 | In vitro enzyme experiments showed that Apatinib was an even more selective inhibitor of VEGFR-2 than sunitinib, with an IC50 of 0.001 μM and 0.005 μM, respectively. Apatinib could also potently suppress the activities of Ret, c-kit, and c-src with an IC50 of 0.013 μM, 0.429 μM, and 0.53 μM, respectively. Apatinib had no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. Apatinib slightly inhibits proliferation of HUVEC stimulated by 20% FBS (IC50: 23.4 μM), whereas Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50: 0.17 μM). The IC50 values of Sunitinib are lower under the same conditions (7.4 μM and 0.034 μM, respectively). 1 μM Apatinib significantly inhibits the migration of HUVEC induced by FBS. At a concentration of 1 μM, Sunitinib also inhibits the migration of HUVEC [1]. Apatinib significantly enhanced the cytotoxicity of ABCB1 or ABCG2 substrate drugs in KBv200, MCF-7/adr, and HEK293/ABCB1 cells overexpressing ABCB1 and in S1-M1-80, MCF-7/FLV1000, and HEK293/ABCG2-R2 cells overexpressing ABCG2 (wild-type). In contrast, apatinib did not alter the cytotoxicity of specific substrates in the parental cells and cells overexpressing ABCC1. Apatinib significantly increased the intracellular accumulation of rhodamine 123 and doxorubicin in the multidrug resistance (MDR) cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [(125)I]iodoarylazidoprazosin in a concentration-dependent manner. The ATPase activity of both ABCB1 and ABCG2 was significantly increased by apatinib. However, apatinib, at a concentration that produced a reversal of MDR, did not significantly alter the ABCB1 or ABCG2 protein or mRNA expression levels or the phosphorylation of AKT and extracellular signal-regulated kinase 1/2 (ERK1/2) [2]. |
体内活性 | Once-daily oral administration of YN968D1 produced a dose-dependent inhibition of tumor growth in all tumor models examined. Statistically significant growth inhibition was obtained with 50 mg/kg?day YN968D1 in three of five tumor xenografts tested. Each tumor xenograft model was significant growth inhibited by YN968D1 at the dose of 100?kg/day. Similar tumor growth inhibition was observed (T?C%, 8% to 18%) in mice following treatment with YN968D1 at the dose of 200?kg/day [1]. There was no significant difference in tumor size between animals treated with saline, apatinib, or paclitaxel. However, the combination of apatinib and paclitaxel produced a significant inhibition of tumor growth compared with animals treated with saline, paclitaxel, or apatinib alone (P<0.05). The ratio of tumor growth inhibition by the combination was 52.7%. Furthermore, at the doses tested, no mortality or apparent decrease in body weight was observed in the combination treatment groups [2]. |
激酶实验 | The inhibitory activity of YN968D1 against tyrosine kinases was determined using ELISA methodology described previously. Her-2, c-kit, and c-src were activated intracellular protein tyrosine kinases expressed by Bab-to-Bac Baculovirus Expression Vector System and purified by Ni-NTA spin columns. The optical density was measured at 490 nm using VERSAmax. The inhibitory activity was expressed as IC50, which was calculated from three independent experiments by the Logit method [1]. |
细胞实验 | Immunohistochemistry was used to determine vessel density by analyzing the expression of CD31, an endothelial marker. Briefly, nude mice xenografted with NCI-H460 tumor were treated with 200 mg/kg Apatinib by the oral garage for 14 days and tumor sections were prepared from formalin-fixed and paraffin-embedded tumor tissues. Slides were treated with 3% H2O2 for 10 min and then incubated in 2% goat serum for 20 min to block the nonspecific antibody binding. Slides were stained with the anti-CD31 antibody at room temperature for 2 h, followed by treatment with biotinylated goat anti-mouse IgG and SABC complex at 37C for 30 min. Finally, diaminobenzidine tetrachloride was used for color development and the slides were counterstained with hematoxylin. Positive cells in images were measured with Image-Pro Plus software [1]. |
动物实验 | The effects of YN968D1 on tumor growth were tested against various human tumors grown subcutaneously in BALB? cA nude mice. Tumor growth was initiated by subcutaneous inoculation of cells into mice. Tumors were allowed to establish and grow to 100–300 mm^3, at which time the mice were randomized into experimental groups. YN968D1 was administered once daily by oral gavage for the indicated periods. In combination treatment experiments, mice were administered YN968D1 alone by oral gavage; 5-FU, oxaliplatin, docetaxel and doxorubicin alone by intravenous injection; or YN968D1 in combination with each cytotoxic drug at the indicated dose and schedule. Tumor volume and body weight were monitored every other day or every 3 days, with the means indicated for groups of six (treated) or 12 (vehicle control) animals. Tumor volumes were determined by measuring the largest diameter (a) and its perpendicular (b) according to the formula (a ×b^2)? 2. The evaluation index for inhibition was the relative tumor growth ratio according to the equation: T?C (%) = mean increase of tumor volumes of treated groups?mean increase of tumor volumes of control groups ×100% [1]. |
别名 | 曲前列尼尔钠, UT-15 |
分子量 | 412.5 |
分子式 | C23H33NaO5 |
CAS No. | 289480-64-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/Ml
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Treprostinil Sodium 289480-64-4 Angiogenesis Apoptosis GPCR/G Protein Immunology/Inflammation Tyrosine Kinase/Adaptors VEGFR c-RET Prostaglandin Receptor 曲前列尼尔钠 UT15 UT-15 inhibit Treprostinil Inhibitor UT 15 inhibitor