1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. 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)。

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TTT-28 Chemical Structure

TTT-28 Chemical Structure

CAS No. : 1609138-51-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥11989
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1 mg ¥3500
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5 mg ¥9500
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (435.80 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7432 mL 8.7160 mL 17.4319 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7432 mL 8.7160 mL 17.4319 mL 43.5798 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 mL 8.7160 mL
10 mM 0.1743 mL 0.8716 mL 1.7432 mL 4.3580 mL
15 mM 0.1162 mL 0.5811 mL 1.1621 mL 2.9053 mL
20 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1790 mL
25 mM 0.0697 mL 0.3486 mL 0.6973 mL 1.7432 mL
30 mM 0.0581 mL 0.2905 mL 0.5811 mL 1.4527 mL
40 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.8716 mL
60 mM 0.0291 mL 0.1453 mL 0.2905 mL 0.7263 mL
80 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.4358 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TTT-28
目录号:
HY-101511
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