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]. |
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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].
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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. |
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| 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 |
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| 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 | 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。 |
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