2. GPCR/G Protein
  3. P2Y Receptor
  4. MRS4917

MRS4917 是一种口服有效的强效选择性 P2Y14 受体 (hP2Y14R) 拮抗剂 (IC50 = 2.88 nM，Ki = 1.67 nM)，其对 P2Y6R 具有超过 18000 倍的选择性 (IC50 = 54 μM)。MRS4917 经口服给药后，可有效逆转慢性坐骨神经压迫 (CCI) 小鼠模型中已形成的机械性痛觉超敏，同时不影响体温调节。MRS4917 可用于神经系统疾病研究。

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MRS4917

MRS4917 Chemical Structure

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Customer Review

MRS4917 相关抗体

Top Publications Citing Use of Products

查看 P2Y Receptor 亚型特异性产品:

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research[1].

IC50 & Target[1]

hP2Y14R

2.88 nM (IC50)

P2Y6 Receptor

54 μM (IC50)

体外研究
(In Vitro)

MRS4917 (compound 11) (0.1-10 μM, 72 小时) 在体外展现出良好的安全性，包括低细胞毒性、对 CYP450 酶 (CYP2D6 与 CYP3A4) 无显著抑制、并且在广泛的脱靶筛选中显示出高选择性 (仅微弱作用于 α2C 受体)[1]。

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

MRS4917 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 and SH-SY5Y cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
Result: Showed low cytotoxicity (18 % growth inhibition) in HepG2 cells at 10 μM.
Induced a slight growth-promoting effect (15 % increase) in SH-SY5Y cells at 10 μM.
体内研究
(In Vivo)

MRS4917 (1.37 mg/kg 单次口服，或 4.58 mg/kg 单次腹腔注射) 可减轻慢性坐骨神经压迫 (CCI) 小鼠模型中的机械性异常疼痛[1]。
MRS4917 (10 mg/kg，单次腹腔注射) 对野生型 C57BL/6J 小鼠的体温或自主活动均无影响[1]。
MRS4917 (10 mg/kg, 腹腔注射，于 MRS2905 给药前 60 分钟注射) 可有效阻断 P2Y14R 激动剂 MRS2905 (5 mg/kg，腹腔注射) 在雄性C57BL/6J小鼠中诱导的低体温效应[1]。

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

Animal Model: Wild-type C57BL/6J male mice[1]
Dosage: 10 mg/kg
Administration: i.p., single dose
Result: Showed no significant effect on core body temperature.
Induced no significant changes in locomotor activity.
Animal Model: Adult male ICR mice with CCI of the left sciatic nerve (Bennett method)[1]
Dosage: 1.37 mg/kg (p.o.) and 4.58 mg/kg (i.p.)
Administration: p.o. and i.p., single dose
Result: Reached full efficacy within 1 hour after both oral and i.p. administration, and maintained this effect over a prolonged period.
The lower oral dose achieved comparable in vivo efficacy to the higher i.p. dose.
Showed no effect on the contralateral (control) paw.
Animal Model: Wild-type C57BL/6J male mice[1]
Dosage: 10 mg/kg
Administration: i.p., 60 min before MRS2905 (5 mg/kg, i.p.)
Result: Blocked the hypothermic effect induced by the P2Y14R agonist MRS2905.
分子量

458.43

Formula

C27H17F3N2O2
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

MRS4917 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:

MRS4917MRS 4917MRS-4917P2Y ReceptorP2Y14RinflammationmechanoallodyniaCCI mouse modelinflammatoryHepG2SH-SY5YInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-178006
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