2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. TMP778

TMP778 是一种有效的、RORγt 的选择性逆向激动剂，其 FRET 检测出的 IC50 值为 7 nM。

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TMP778 Chemical Structure

TMP778 Chemical Structure

CAS No. : 1422053-04-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4900
In-stock
1 mg ￥2045
In-stock
5 mg ￥4500
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

Other Forms of TMP778:

TMP778 相关抗体

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RORγ RORα RORβ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.

IC50 & Target

IC50: 7 nM (FRET assay), 63 nM (IL-17F promoter assay), 0.03 μM (in Th17 cells), 0.005 μM (in Tc17 cells)[1].
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Jurkat IC50
63 nM
Compound: 8; TMP778
Inverse agonist activity at RORgamma (unknown origin) expressed in human Jurkat cells assessed as inhibition of IL-17F production after 20 hrs by luciferase reporter gene assay
Inverse agonist activity at RORgamma (unknown origin) expressed in human Jurkat cells assessed as inhibition of IL-17F production after 20 hrs by luciferase reporter gene assay
[PMID: 27542308]
体外研究
(In Vitro)

It is found that TMP778 at >2.5 μM starts to show toxic effects on cell growth, which however is not RORγt-dependent, since the proliferation of RORγt-deficient T cells cultured under Th17 cell-polarizing conditions is also decreased. Otherwise, these inhibitors do not show inhibitory effects on cell proliferation or RORγt expression or its nuclear translocation, but efficiently inhibited IL-17 production. TMP778 has a much broader dose range and efficiently decreased IL-17 production, consistent with its higher binding affinity for RORγt. These data indicate that TMP778 is the RORγt inhibitor that most potently reduced IL-17 production[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TMP778 相关抗体:
体内研究
(In Vivo)

All three compounds (e.g., TMP778) delay the onset of disease and substantially reduce the severity of disease progression compared to control-treated mice. Consistent with in vitro results, TMP778 treatment causes the most pronounced effect on the disease phenotype. This treatment not only decreases the number of mononuclear cells infiltrating the central nervous system (CNS), but also most strongly reduces the percentage of IL-17+ T cells in the CNS (including IL-17+ IFNγ+). There is no significant change in the percentage IFNγ+ IL-17-T cells in the CNS among all groups, indicating that none of the inhibitors affects Th1 responses. TMP778 strongly inhibits Th17 cell generation, reduces IL-17 production from differentiated Th17 cells, and also dramatically ameliorates the progression of EAE[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

494.58

Formula

C31H30N2O4
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
细胞实验： 

DMSO 中的溶解度 : 240 mg/mL (485.26 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 2.0219 mL 10.1096 mL 20.2192 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 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

只
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
Cell Assay
[2]

Naive CD4+ T cells are activated in 96-well plates under Th17 cell polarizing conditions in the presence of indicated doses of RORγt inhibitors (e.g., TMP778: 30, 10, 2.5, 0.83, 0.28, 0.09 μM ) or vehicle control DMSO. After 48 h, plates are pulsed for 16 h with 1 μCi 3H-thymidine per well. Proliferation is measured as counts per minute by using a Wallac Liquid Scintillation Counter[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
EAE is induced in C57BL/6 mice with MOG35-55 plus CFA immunization in conjunction with subcutaneous administration of the inhibitors twice daily from day 0. C57BL/6 mice are immunized with MOG35-55 plus CFA, and RORγt inhibitor (TMP778, 200 μg per injection, n=19; TMP920, 500 μg per injection, n=7; Digoxin, 50 μg per injection, n=5, >100 μg cause mouse death; DMSO, n=19) are subcutaneously injected twice daily starting from day 0. Mice are evaluated daily for signs of EAE. When 11 days after groups of mice treated with different RORγt inhibitors are compared with the group of mice with DMSO (vehicle control) treatment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

TMP778 相关分类

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 2.0219 mL 10.1096 mL 20.2192 mL 50.5479 mL
5 mM 0.4044 mL 2.0219 mL 4.0438 mL 10.1096 mL
10 mM 0.2022 mL 1.0110 mL 2.0219 mL 5.0548 mL
15 mM 0.1348 mL 0.6740 mL 1.3479 mL 3.3699 mL
20 mM 0.1011 mL 0.5055 mL 1.0110 mL 2.5274 mL
25 mM 0.0809 mL 0.4044 mL 0.8088 mL 2.0219 mL
30 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6849 mL
40 mM 0.0505 mL 0.2527 mL 0.5055 mL 1.2637 mL
50 mM 0.0404 mL 0.2022 mL 0.4044 mL 1.0110 mL
60 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 mL
80 mM 0.0253 mL 0.1264 mL 0.2527 mL 0.6318 mL
100 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5055 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.

Keywords:

TMP7781422053-04-0TMP 778TMP-778RORRAR-related orphan receptorInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-102075A
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