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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-MARY1
MARY1

Chemical Structure : MARY1

CAS No.:

MARY1

货号: PC-24891Not For Human Use, Lab Use Only.

MARY1 is potent, and selective 5-hydroxytryptamine 2B receptor (5-HT2BR) antagonist with Ki of 764 nM, induces mitochondrial biogenesis (MB) enhances mitochondrial function in the kidney.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MARY1 is potent, and selective 5-hydroxytryptamine 2B receptor (5-HT2BR) antagonist with Ki of 764 nM, induces mitochondrial biogenesis (MB) enhances mitochondrial function in the kidney.
MARY1 shows no significant binding to 5-HT2A/2C receptors.
MARY1 selectively antagonizes the 5-HT2BR (IC50 = 381 nM; Emax = 90%), with no activity against 5-HT2A or 5-HT2C receptors.
MARY1 (1 nM-1 uM) enhances cellular mitochondrial maximal respiration, upregulates key genes responsible for mitochondrial bioenergetics, and increases the mitochondrial number in RPTCs, indicating MB, in primary rabbit renal proximal tubule cells (RPTCs).
MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in vitro.
MARY1 (0.3 mg/kg, i.p.) induces MB in the renal cortex in vivo, resulted in increased PGC-1α and sirtuin 1 (SIRT1) mRNA, and mtDNA content (DLOOP and mtND1) in the renal cortex of control mice.

物理化学性质&存储条件

分子量 378.36
分子式 C18H17F3N4O2
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

2,4,6-trifluoro-N-(6-(4-methylpiperazine-1-carbonyl)pyridin-2-yl)benzamide

参考文献

1. Santiago Raj PV, et al. ACS Pharmacol Transl Sci. 2025 May 30;8(6):1741-1755.

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