TTT-28

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TTT-28 

TTT-28 是一种噻唑-缬氨酸肽模拟物,高效 ABCB1 (P-gp/MDR1) 选择性抑制剂,低毒性。TTT-28 通过选择性阻断 ATP 结合盒亚家族 B 成员1 (ABCB1) 的外排功能, 逆转ABCB1介导的多药耐药性 (MDR)。

TTT-28

TTT-28 Chemical Structure

CAS No. : 1609138-51-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1[1].

体外研究
(In Vitro)

TTT-28 (0-100 μM; 72 hours) reverses ABCB1-mediated MDR in drug selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells; the IC50s of TTT-28 in CCD-18Co, SW620 and SW620/Ad300 cells are 213.4±11.0 μM, 89.4±3.9 μM and 92.0±5.0 μM, respectively[1].
TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells[1].
TTT-28 (10 μM; 0-72 hours) does not interfer with the expression level and localization of ABCB1, it results from blocking the efflux function of ABCB1[1].
TTT-28 (0-40 μM; 2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SW620 cells, SW620/Ad300 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 72 hours
Result: Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells.

体内研究
(In Vivo)

TTT-28 (deliver orally; 30 mg/kg; every 3 rd day; 18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1, it enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage: 30 mg/kg
Administration: Deliver orally; every 3rd day; 18 days
Result: Lead to higher intratumoral accumulation of paclitaxel in tumors.

分子量

573.66

Formula

C31H31N3O6S

CAS 号

1609138-51-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Wang YJ, et al. Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCB1. Sci Rep. 2017 Feb 9;7:42106.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务