2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. 5-HT Receptor PGC-1α Akt PI3K Ras MEK ERK
  4. MARY1

MARY1 是一种选择性 5-HT2BR 拮抗剂，IC50 为 380 nM，Ki 为 764 nM (人类 5-HT2BR)。MARY1 可诱导肾脏线粒体的生物合成 (MB) 并通过增加肾近端小管细胞 (RPTC) 的线粒体呼吸能力、线粒体蛋白水平和线粒体数量增强肾脏的线粒体功能。MARY1 通过 5-HT2BR 和双重 PI3K/AKT 和 RAS/MEK/ERK 细胞信号通路在 RPTCs 中诱导 MB。MARY1 可用于研究代谢和线粒体功能障碍相关的肾脏疾病。

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MARY1

MARY1 Chemical Structure

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MARY1 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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K-Ras H-Ras N-Ras Ras

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human 5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction[1].

IC50 & Target[1]

5-HT2B Receptor

380 nM (IC50)

human 5-HT2B Receptor

761 nM (Ki)

体外研究
(In Vitro)

MARY1 与 5-HT2BR 具有中等亲和力，与 5-HT2A/2C 受体无显著结合[1]。

MARY1 (1 nM-1 μM，24 小时) 可增加 RPTCs 中的线粒体最大呼吸作用[1]。

MARY1 (1 nM，24 小时) 可增强细胞线粒体最大呼吸作用，上调线粒体生物能量学关键基因的表达，并增加 RPTCs 中的线粒体数量[1]。

MARY1 可增加 scRNA 处理的 RPTCs 中的 PGC-1α 表达，但不会增加 siRNA 处理的 RPTCs 中的 PGC-1α 表达[1]。

MARY1 (1 nM，20 分钟) 通过 5-HT2BR 和 PI3K/AKT 双信号通路以及 RAS/MEK/ERK 双信号通路诱导 RPTCs 中的 MB[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MARY1 相关抗体:

Western Blot Analysis[1]

Cell Line: RPTCs
Concentration: 1 nM
Incubation Time: 24 h
Result: Increased the protein levels of mitochondrial-specific genes in RPTCs, including carnitine palmitoyltransferase 1A (CPT1A), acyl-CoA synthetase medium-chain family member 2A (ACSM2A), and NADH dehydrogenase [ubiquinone] 1β subcomplex subunit 8 (NDUFB8).

Western Blot Analysis[1]

Cell Line: RPTCs
Concentration: 1 nM
Incubation Time: 20 min
Result: Increased pAKT (S473) and pFOXO1 (S256) .
Activated RAS GTPase and activated phosphorylation of extracellular signal-regulated kinase (pERK) at the threonine 202/tyrosine 204 (T202/Y204) position.
体内研究
(In Vivo)

MARY1 (0.3 mg/kg，腹腔注射，一次) 在雄性 C57BL/6NCrl 小鼠的肾皮质中诱导 MB[1]。

MARY1 (0.15-0.3 mg/kg，腹腔注射，一次) 在雄性 SD 大鼠的肾皮质中诱导 MB[1]。

MARY1 (0.15-15 mg/kg，腹腔注射，每日一次，4 周) 不会导致雄性 SD 大鼠死亡或器官及体重异常[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6NCrl mice 8 weeks of age and weighing ∼20-25 g[1]
Dosage: 0.3 mg/kg
Administration: i.p.,once
Result: Increased PGC-1α and sirtuin 1 (SIRT1) mRNA, and mtDNA content (DLOOP and mtND1) in the renal cortex, with no effect on mitochondrial transcription factor A.
Upregulated nuclear (3.46-fold), but not cytosolic PGC-1α in the renal cortex.
Increased ACSM2A (1.75-fold), NDUFB8 (1.52-fold), and stearoyl-CoA desaturase 1 (SCD1; 1.65-fold) proteins.
Increased complex I (NDUFB8) and II (SDHB) proteins of the mitochondrial electron transport chain, with no changes in complexes III (UQCRC2), IV (MTCO1), or V (ATP5A)
Increased mitochondrial fission proteins mitochondrial fission factor (Mff; 1.79-fold) and dynamin-related protein 1 (Drp1; 2.01-fold) in the mouse renal cortex, but not mitochondrial fusion proteins mitofusin 1 (MFN1) and 2 (MFN2), and did not alter TFAM protein levels.
Animal Model: Male SD rats(weighing 250-300 g) [1]
Dosage: 0.15 mg/kg, 0.3 mg/kg
Administration: i.p., once
Result: Increased PGC-1α protein levels in the renal cortex at both doses.
Animal Model: Male SD rats(weighing 250-300 g) [1]
Dosage: 0.15 mg/kg, 1.5mg/kg, 15 mg/kg
Administration: i.p., once a day, 4 weeks
Result: Did not cause any death or organ and weight abnormalities.
分子量

378.35

Formula

C18H17F3N4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MARY1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MARY1MARY 1MARY-15-HT ReceptorPGC-1αAktPI3KRasMEKERKSerotonin Receptor5-hydroxytryptamine ReceptorPPARγ coactivator-1αPKBProtein kinase BPhosphoinositide 3-kinaseMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesAntagonistKidney diseaseRPTCs5-HT2BRPI3K/AKTRAS/MEK/ERKInhibitorinhibitorinhibit

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