MIPS521

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MIPS-521 是 A1R 的正变构调节剂。

MIPS-521 is a positive allosteric modulator of the A1R.

MIPS521 (compound 13o) (3-10 μM) improves the ability of R-PIA to promote A1AR-mediated ERK1/2 phosphorylation.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.

MIPS521 (1-30 μg in 10 μL; intrathecal administration) reverses mechanical hyperalgesia in rats, promoting robust antinociception.MIPS521 (10 μg in 10 μL; intrathecal administration) significantly reduces spontaneous pain in a conditioned place preference model.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. Animal Model:Male and female Sprague-Dawley rats (7-12 weeks) were performed a partial nerve ligation (PNL) or sham surgery 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.

MIPS-521 | {2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone

Apoptosis

Adenosine Receptor

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1146188-19-3

449.8

C19H10ClF6NOS

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (55.58 mM)

Nc1c(C(c(cc2)ccc2Cl)=O)c(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1

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(-20℃)

With Ice Pack

≥ 2 years