2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. ML00253764

ML00253764 是一种选择性的黑皮质素受体 4 (MC4R) 拮抗剂，可以通过抑制 ERK1/2 和 Akt 磷酸化诱导细胞凋亡 (apoptosis)，具有抗癌活性。

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ML00253764 Chemical Structure

ML00253764 Chemical Structure

CAS No. : 681847-92-7

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1650
In-stock
1 mg ￥681
In-stock
5 mg ￥1500
In-stock
10 mg ￥2500
In-stock
25 mg ￥4400
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of ML00253764:

ML00253764 相关抗体

Top Publications Citing Use of Products

查看 Melanocortin Receptor 亚型特异性产品:

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MC1R MC3R MC2R MC4R MC5R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
1030 nM
Compound: 5
Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
160 nM
Compound: 5
Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
2708 nM
Compound: 5
Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
2860 nM
Compound: 5
Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
2900 nM
Compound: 5
Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
355 nM
Compound: 5
Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
3770 nM
Compound: 5
Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
560 nM
Compound: 5
Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
6190 nM
Compound: 5
Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 IC50
708 nM
Compound: 5
Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
体外研究
(In Vitro)

ML00253764(0.001-50 μM, 24 h or 72 h)对人胶质母细胞瘤细胞增殖具有显著的时间和浓度依赖性抑制活性，其中作用于 U-118 细胞的 IC50 值为 6.56 μM，可以诱导U-87细胞凋亡，且在这两种细胞系中均表现出显著的 ERK1/2 磷酸化抑制作用[1]。

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

ML00253764 相关抗体:
体内研究
(In Vivo)

ML00253764(30 mg/kg, s.c., daily, 34 days) 可抑制感染 U-87 细胞的 CD nu/nu 雄性小鼠肿瘤生长[1]。

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

377.25

Formula

C18H18BrFN2O
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 : 66.67 mg/mL (176.73 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 2.6508 mL 13.2538 mL 26.5076 mL
5 mM 0.5302 mL 2.6508 mL 5.3015 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

ML00253764 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 2.6508 mL 13.2538 mL 26.5076 mL 66.2691 mL
5 mM 0.5302 mL 2.6508 mL 5.3015 mL 13.2538 mL
10 mM 0.2651 mL 1.3254 mL 2.6508 mL 6.6269 mL
15 mM 0.1767 mL 0.8836 mL 1.7672 mL 4.4179 mL
20 mM 0.1325 mL 0.6627 mL 1.3254 mL 3.3135 mL
25 mM 0.1060 mL 0.5302 mL 1.0603 mL 2.6508 mL
30 mM 0.0884 mL 0.4418 mL 0.8836 mL 2.2090 mL
40 mM 0.0663 mL 0.3313 mL 0.6627 mL 1.6567 mL
50 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
60 mM 0.0442 mL 0.2209 mL 0.4418 mL 1.1045 mL
80 mM 0.0331 mL 0.1657 mL 0.3313 mL 0.8284 mL
100 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6627 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:

ML00253764681847-92-7ML 00253764ML-00253764Melanocortin ReceptorMC ReceptorMC4RERK1/2AktapoptosisanticancerInhibitorinhibitorinhibit

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产品名称：
ML00253764
目录号：
HY-124740
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