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首页-小分子抑制剂&激动剂-Others-Other Targets-MS0015203
MS0015203

Chemical Structure : MS0015203

CAS No.: 73912-52-4

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MS0015203 (MS15203, MS 0015203)

货号: PC-47110Not For Human Use, Lab Use Only.

MS0015203 (MS15203) is a potent, selective small-molecule agonist of neuropeptide receptor GPR171 with binding IC50 of 81 nM (WT GPR171).

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥2980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MS0015203 (MS15203) is a potent, selective small-molecule agonist of neuropeptide receptor GPR171 with binding IC50 of 81 nM (WT GPR171).
MS0015203 displays high selectivity against a panel of 80 other membrane proteins, including family A GPCRs.
MS0015203 potently binds to the mutants receptors (Y99A, Y239A, and R243A) except C184A.
MS0015203 dose-dependently increased [35S]GTPγS binding and inhibited adenylyl cyclase activity in rat hypothalamic membranes (EC50=5.0 nM).
Systemic or central administration of MS0015203 increased feeding through a mechanism involving GPR171.
MS0015203 (3 mg/kg, intraperitoneally) caused a significant increase in the total number of c-Fos–positive cells, increase in neuronal activity within cells containing GPR171 in the paraventricular nucleus (PVN) in mice.
Administration of MS0015203 (2.5 mg/kg, 40 days) significantly increased the abundance of the mRNAs encoding proSAAS, NPY, AgRP, or orexin in the ventral hypothalamus, also significantly increased the abundance of the mRNAs encoding the NPY receptor Y1R and the orexin receptor HCRT2 and significantly decreased that encoding the orexin receptor HCRT1 in the ventral hypothalamus.

物理化学性质&存储条件

分子量 249.222
分子式 C12H11NO5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-methacrylamidoisophthalic acid

参考文献

1. Wardman JH, et al. Sci Signal. 2016 May 31;9(430):ra55.

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