1. GPCR/G Protein
  2. Adenosine Receptor
  3. MIPS521

MIPS521 是腺苷受体 (A1AR) 的正向变构调节剂。MIPS521 还具有较低的 A1AR 变构亲和力 (pKB=4.95; KB=11 μM)。MIPS521 通过调节大鼠脊髓中内源性腺苷水平的升高,在体内表现出减轻疼痛的作用。

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MIPS521 Chemical Structure

MIPS521 Chemical Structure

CAS No. : 1146188-19-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥990
In-stock
1 mg ¥342
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5 mg ¥900
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10 mg ¥1400
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50 mg ¥4200
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100 mg ¥6500
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500 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine[1][2].

IC50 & Target[1]

A1AR

 

体外研究
(In Vitro)

MIPS521 (compound 13o) (3-10 μM) improves the ability of R-PIA to promote A1AR-mediated ERK1/2 phosphorylation[1].
MIPS521 (0.3-30 μM; pretreament for 10 min, co-treatment for 30 min) produces a concentration-dependent potentiation of signalling by ADO in an inhibition of cAMP assay (expressed as a percentage of the inhibition of 3 μM forskolin-mediated cAMP) in CHO cells[2].

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

体内研究
(In Vivo)

MIPS521 (1-30 μg in 10 μL; intrathecal administration) reverses mechanical hyperalgesia in rats, promoting robust antinociception[2].
MIPS521 (10 μg in 10 μL; intrathecal administration) significantly reduces spontaneous pain in a conditioned place preference model[2].
MIPS521 (1-30 μg in 10 μL; intrathecal administration) reduces eEPSCs in spinal cord from nerve-injured rats, with a pEC50 of 6.9. The maximum MIPS521-induced decrease in synaptic current amplitude is significantly greater in nerve-injured rats than in sham surgery controls[2].

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

Animal Model: Male and female Sprague-Dawley rats (7-12 weeks) were performed a partial nerve ligation (PNL) or sham surgery[2]
Dosage: 1, 3, 10, 30 μg in 10 μL
Administration: Intrathecal administration
Result: Reduced eEPSCs in spinal cord from nerve-injured rats and reversed mechanical hyperalgesia.
分子量

449.80

Formula

C19H10ClF6NOS

CAS 号
性状

固体

颜色

Light yellow to green 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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 25 mg/mL (55.58 mM; 超声助溶 (<60°C); 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 2.2232 mL 11.1161 mL 22.2321 mL
5 mM 0.4446 mL 2.2232 mL 4.4464 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

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

MIPS521 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 2.2232 mL 11.1161 mL 22.2321 mL 55.5803 mL
5 mM 0.4446 mL 2.2232 mL 4.4464 mL 11.1161 mL
10 mM 0.2223 mL 1.1116 mL 2.2232 mL 5.5580 mL
15 mM 0.1482 mL 0.7411 mL 1.4821 mL 3.7054 mL
20 mM 0.1112 mL 0.5558 mL 1.1116 mL 2.7790 mL
25 mM 0.0889 mL 0.4446 mL 0.8893 mL 2.2232 mL
30 mM 0.0741 mL 0.3705 mL 0.7411 mL 1.8527 mL
40 mM 0.0556 mL 0.2779 mL 0.5558 mL 1.3895 mL
50 mM 0.0445 mL 0.2223 mL 0.4446 mL 1.1116 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.

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产品名称:
MIPS521
目录号:
HY-139644
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