MARY1
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.
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- Formule: C18H17F3N4O2
- Masse moléculaire:378.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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5-HT2B Receptor 380 nM (IC50) |
human 5-HT2B Receptor 761 nM (Ki) |
MARY1 binds with moderate affinity to 5-HT2BR, with no significant binding to 5-HT2A/2C receptors[1].
MARY1 (1 nM-1 μM, 24 h) increase maximal mitochondrial respiration in RPTCs[1].
MARY1 (1 nM, 24 h) enhances cellular mitochondrial maximal respiration, upregulates key genes responsible for mitochondrial bioenergetics, and increases the number of mitochondria in RPTCs[1].
MARY1 increases PGC-1α expression in RPTCs treated with scRNA but not in those treated with siRNA[1].
MARY1 (1 nM, 20 min) induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RPTCs
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Concentration:1 nM
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Incubation Time:24 h
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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).
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Cell Line:RPTCs
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Concentration:1 nM
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Incubation Time:20 min
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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.
| Species | Dose | Route | AUC0-t | Cmax | Tmax | T1/2 | Vz-F_obs | ClF_obs |
|---|---|---|---|---|---|---|---|---|
| Mice | 0.3 mg/kg | i.v. | 19.8 ng·h/mL | 11.9 ng/mL | 0.5 h | 1.22 h | 26785.2 mL/kg | 15145.3 mL/h/kg |
| Mice | 0.3 mg/kg | s.c. | 22.9 ng·h/mL | 27.2 ng/mL | 0.5 h | 1.16 h | 22043.6 mL/kg | 13074.6 mL/h/kg |
MARY1 (0.3 mg/kg, i.p.,once) induces MB in the renal cortex in male C57BL/6NCrl mice[1].
MARY1 (0.15-0.3 mg / kg, i.p., once) induces MB in the renal cortex in Male SD rats[1].
MARY1 (0.15-15 mg/kg, i.p., once a day, 4 weeks) does not cause any death or organ and weight abnormalities in male SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6NCrl mice 8 weeks of age and weighing ∼20-25 g[1]
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Dosage:0.3 mg/kg
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Administration:i.p.,once
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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.
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Animal Model:Male SD rats(weighing 250-300 g) [1]
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Dosage:0.15 mg/kg, 0.3 mg/kg
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Administration:i.p., once
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Result:Increased PGC-1α protein levels in the renal cortex at both doses.
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Animal Model:Male SD rats(weighing 250-300 g) [1]
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Dosage:0.15 mg/kg, 1.5mg/kg, 15 mg/kg
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Administration:i.p., once a day, 4 weeks
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Result:Did not cause any death or organ and weight abnormalities.
Chemical Information
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Masse moléculaire 378.35
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Formule C18H17F3N4O2
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SMILES
FC1=C(C(F)=CC(F)=C1)C(NC2=NC(C(N3CCN(CC3)C)=O)=CC=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MARY1 Related Classifications
HY-174306 Related Classifications
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