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

Dersimelagon  (Synonyms: MT-7117)

目录号: HY-109114 纯度: 97.01%
COA 产品使用指南

摩尔计算器

Dersimelagon (MT-7117) 是一种具有口服活性的选择性黑皮质素 1 受体(MC1R) 激动剂，对人 (h)、食蟹猴 (cm)、小鼠 (m) 和大鼠 (r) MC1R 的 EC50 值分别为 8.16、3.91、1.14 和 0.251 nM。Dersimelagon 对 hMC1R 和 hMC4R 表现出良好的亲和力，Ki 值分别为 2.26 和 32.9 nM。Dersimelagon可用于皮肤色素沉着的研究。

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Dersimelagon Chemical Structure

Dersimelagon Chemical Structure

CAS No. : 1835256-48-8

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10 mg ￥3565
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Customer Review

Dersimelagon 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

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation[1][2].

IC50 & Target[1]

hMC1R

2.26 nM (Ki)

hMC4R

32.9 nM (Ki)

hMC5R

486 nM (Ki)

hMC3R

1420 nM (Ki)

hMC1R

8.16 nM (EC50)

hMC4R

79.6 nM (EC50)

hMC2R

>10000 nM (EC50)

rMC1R

0.251 nM (EC50)

mMC1R

1.14 nM (EC50)

cmMC1R

3.91 nM (EC50)

体外研究
(In Vitro)

Dersimelagon (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) increases eumelanin production in a concentration-dependent manner, with EC50 of 13 pM in B16F1 cells[1].

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

Dersimelagon 相关抗体:
体内研究
(In Vivo)

Dersimelagon (0.003, 0.03, 0.3, 3 mg/kg; p.o. for 6 days) induces coat colour darkening in Ay/a mice in 0.3 and 3 mg/kg[1].
Dersimelagon (0.03, 0.3, 3 mg/kg; p.o.; single administration) upregulates the expression of Tyr, Trp1 and Dct of Ay/a mice at 24, 48 and 72 h in the 3 mg/kg[1].
Dersimelagon (1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks; p.o.) induces pigmentation in a dose-dependent manner, and it is reverses after cessation of administration in cynomolgus monkeys[1].

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

Animal Model: Cynomolgus monkeys[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: P.o.; 1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks
Result: Induced pigmentation in a dose-dependent manner.
Minimum pigmentation effective dose was 1 mg/kg.
Pigmentation diminished 4 weeks after cessation of treatment in the 1, 3 and 10 mg/kg groups and 16 weeks after cessation in the 30 mg/kg group.
Clinical Trial
分子量

675.75

Formula

C36H45F4N3O5
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 97.35%

COA (201 KB) HNMR (288 KB) RP-HPLC (157 KB)

产品使用指南 (1538 KB)
参考文献

Dersimelagon 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

Dersimelagon1835256-48-8MT-7117MT7117MT 7117Melanocortin ReceptorMC Receptorhumancynomolgus monkeymouseratskin pigmentationInhibitorinhibitorinhibit

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