2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. TC-MCH 7c

TC-MCH 7c 是一种苯基吡啶酮衍生物，一种口服有效的，选择性的且可穿透血脑屏障的 MCH1R 拮抗剂，对 hMCH1R 的 IC50 为 5.6 nM。TC-MCH 7c 对人和小鼠 MCH1R 的 Ki 分别为 3.4 nM 和 3.0 nM。

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TC-MCH 7c Chemical Structure

TC-MCH 7c Chemical Structure

CAS No. : 864756-35-4

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规格 价格 是否有货
10 mM * 1 mL in DMSO ￥5257
询问价格 & 货期
1 mg ￥1950
询问价格 & 货期
5 mg ￥5850
询问价格 & 货期

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Customer Review

TC-MCH 7c 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R[1]. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively[2].

IC50 & Target

IC50: 5.6 nM (hMCH1R)[1]
Ki: 3.4 nM (hMCH1R) and 3.0 nM (mouse MCH1R)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
23 nM
Compound: 7c
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
[PMID: 21190859]
CHO IC50
5.6 nM
Compound: 7c
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
[PMID: 21190859]
CHO-K1 IC50
5.6 nM
Compound: 1
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
[PMID: 19632840]
体外研究
(In Vitro)

TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca2+]i mobilization[1].
TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively[2].

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

TC-MCH 7c 相关抗体:
体内研究
(In Vivo)

TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model[1].
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively[2].

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

Animal Model: C57BL/6J DIO mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Oral; once-daily for 1.5 months
Result: Exhibited excellent body weight reduction in a dose-dependent manner.
Animal Model: Diet-induced obesity mice[2]
Dosage: 3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.
分子量

408.47

Formula

C24H25FN2O3
CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 20 mg/mL (48.96 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 2.4482 mL 12.2408 mL 24.4816 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

TC-MCH 7c 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4482 mL 12.2408 mL 24.4816 mL 61.2040 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 mL 12.2408 mL
10 mM 0.2448 mL 1.2241 mL 2.4482 mL 6.1204 mL
15 mM 0.1632 mL 0.8161 mL 1.6321 mL 4.0803 mL
20 mM 0.1224 mL 0.6120 mL 1.2241 mL 3.0602 mL
25 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4482 mL
30 mM 0.0816 mL 0.4080 mL 0.8161 mL 2.0401 mL
40 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5301 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:

TC-MCH 7c864756-35-4MCHR1 (GPR24)Melanin concentrating hormone receptor 1orallyavailablebrain-penetrableMCHObesityphenylpyridonederivativeInhibitorinhibitorinhibit

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