货号	规格	价格	上海	北京	珠海	重庆	武汉
S89009-5mg买3赠1	99.90%	￥430.00 S89009-5mg ￥430.00 现货（买3赠1）	5 5	-	-	-	-
S89009-10mg买3赠1	99.90%	￥690.00 S89009-10mg ￥690.00 现货（买3赠1）	6 6	-	-	-	-
S89009-25mg促销	99.90%	￥1330.00 ￥1060.00 S89009-25mg ￥1060.00 现货	6 6	-	-	-	-
S89009-100mg促销	≥98%	￥3390.00 ￥2710.00 S89009-100mg ￥2710.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM

靶点：

EC50: 190 nM (MRGPRX1)

体外研究：

In the absence of ML382, the IC50 for BAM8-22 inhibition of ICa is 0.66 ± 0.05 μM. In the presence of 0.1 μM, 1 μM, 10 μM, and 30 μM ML382, BAM8-22 IC50 is reduced to 0.43 ± 0.02 μM, 0.25 ± 0.02 μM, 0.06 ± 0.01 μM, and 0.08 ± 0.01 μM, respectively. A lower IC50 generally indicates a higher potency; thus, ML382 dose-dependently increases the potency of BAM8–22, further demonstrating that ML382 is a positive allosteric modulator of MRGPRX1

体内研究：

ML382 (5 μM) significantly increases inhibition of ICa by a low concentration of BAM8–22 (0.5 μM) in DRG neurons from MrgprX1 mice. ML382 enhances the inhibition of spinal synaptic transmission by BAM8-22 in MrgprX1 mice. ML382 (25 μM, 125 μM, and 250 μM; 5 μL; i.th.;) dose-dependently attenuates heat hypersensitivity in MrgprX1 mice. ML382 (lumbar puncture injection; 25 μM, 5 μL) leads to a significant increase in postconditioning time spent in the ML382-paired chamber, compared with the preconditioning value. ML382 inhibits nerve injury-induced ongoing pain in MrgprX1 mice

参考文献：

1. Li Z, et al. Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain. Proc Natl Acad Sci U S A. 2017;114(10):E1996-E2005. 2. Wen W, et al. Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1. ChemMedChem. 2015;10(1):57-61.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.774 ml	13.872 ml	27.745 ml
5 mM	0.555 ml	2.774 ml	5.549 ml
10 mM	0.277 ml	1.387 ml	2.774 ml
50 mM	0.055 ml	0.277 ml	0.555 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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ML 382