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MIPS521
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MIPS521图片
CAS NO:1146188-19-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

MIPS521 is a positive allosteric modulator ofadenosine A1receptor(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].

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 pEC50of 6.9. The maximum MIPS521-induced decrease in synaptic current amplitude is significantly greater in nerve-injured rats than in sham surgery controls[2].

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

性状

Solid

Formula

C19H10ClF6NOS

CAS 号

1146188-19-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(55.58 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2232 mL11.1161 mL22.2321 mL
5 mM0.4446 mL2.2232 mL4.4464 mL
10 mM0.2223 mL1.1116 mL2.2232 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。