1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. MK-8768

MK-8768是一种口服有效的,可透过血脑屏障的选择性 mGluR2 负变构调节剂 (IC50 为 9 nM)。

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MK-8768 Chemical Structure

MK-8768 Chemical Structure

CAS No. : 1432729-22-0

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.

IC50 & Target

IC50:9.6 nM(mGluR2)[1]

体外研究
(In Vitro)

MK-8768 (40 n M, 5 min) 在过表达 mGluR2 的 CHOdhfr 细胞系中抑制 mGluR2 酶活,IC50值为0.9 nM[1]

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

Cell Viability Assay

Cell Line: CHOdhfr- cells expressing human mGluR2[1]
Concentration: 40 nM
Incubation Time: 5 min
Result: Inhibits the viability of mGluR2.
体内研究
(In Vivo)

MK-8768 优先采用肌肉注射[1]
MK-8768 (3 mg/kg, i.m, 2 times weekly) 在恒河猴ORD模型中明显改善东莨菪碱损伤后的影响,维持良好的执行功能和注意力[1]

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

Animal Model: Rhesus monkey ORD model[2]
Dosage: 3 mg/kg
Administration: Intramuscular (i.m.), 2 times weekly
Result: Improved object retrieval following scopolamine impairment obviously at the concentration of 0.3 mg/ml.
分子量

433.43

Formula

C21H22F3N5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 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 *
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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.

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产品名称:
MK-8768
目录号:
HY-155088
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