MIPS521

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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。

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 (pK_B=4.95; K_B=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 (pK_B=4.95; K_B=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°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 : 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 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
10 mM	0.2223 mL	1.1116 mL	2.2232 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。