MK-0354
Based on 2 publication(s) in Google Scholar
MK-0354 is a specific GPR109a receptor agonist with EC50 values of 1.65 μM and 1.08 μM for hGPR109a and mGPR109a, respectively. MK-0354 can be used in liver cancer research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 851776-28-8
- Formel: C7H8N6
- Molecular Weight:176.18
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) MK-0354
More
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Adipocyte | IC50 |
0.87 μM
Compound: MK-0354
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Antidyslipidemic activity in human adipocytes assessed as inhibition of isoproteranol-induced production of free fatty acids
Antidyslipidemic activity in human adipocytes assessed as inhibition of isoproteranol-induced production of free fatty acids
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[PMID: 20363624] |
| Adipocyte | IC50 |
3.1 μM
Compound: 5a, MK-0354
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Inhibition isoproterenol-stimulated lipolysis in human adipocytes
Inhibition isoproterenol-stimulated lipolysis in human adipocytes
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[PMID: 18665582] |
| CHO | EC50 |
0.286 μM
Compound: MK-0354
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Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
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[PMID: 20363624] |
| CHO | EC50 |
286 nM
Compound: 1, MK-0354
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Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
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[PMID: 22435740] |
MK-0354 (200 μM) fails to induce the recruitment of β-arrestin1-mYFP to the cell membrane of cells expressing GPR109A β-arrestin1-mYFP[3].
MK-0354 (50 μM; 12 h) has no impact on CM-mediated GPR109A upregulation, NF-κB axis activation, or immunosuppressive polarization of tumor-associated myeloid cells (G-MDSC and BMDM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 851776-28-8
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Appearance Solid
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Molecular Weight 176.18
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Formel C7H8N6
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Color Light yellow to khaki
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SMILES
C12=C(CCC2)C(C3=NN=NN3)=NN1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Early life gut microbiota sustains liver-resident natural killer cells maturation via the butyrate-IL-18 axis. [Abstract]2023 Mar 27;14(1):1710. PMID: 36973277 -
iScience
Comparative analysis reveals molecular adaptation of mammalian HCA2 to microbial metabolites. [Abstract]2026 May 22;29(6):116030. PMID: 42221821
Lösungsmittel & Löslichkeit
DMSO : ≥ 36 mg/mL (204.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (14.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Semple G, et al. 3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice. J. Med. Chem., 2008, 51 (16), pp 5101-5108 [Content Brief]
[2]. Lai E1, et al. Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans. J Clin Lipidol. 2008 Oct;2(5):375-383. [Content Brief]
[3]. Walters RW, et al. beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice. J Clin Invest. 2009 May;119(5):1312-21. [Content Brief]
[4]. Yang Y, et al. Dietary vitamin B3 supplementation induces the antitumor immunity against liver cancer via biased GPR109A signaling in myeloid cell. Cell Rep Med. 2024 Sep 17;5(9):101718. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.6760 mL | 28.3801 mL | 56.7601 mL | 141.9003 mL |
| 5 mM | 1.1352 mL | 5.6760 mL | 11.3520 mL | 28.3801 mL | |
| 10 mM | 0.5676 mL | 2.8380 mL | 5.6760 mL | 14.1900 mL | |
| 15 mM | 0.3784 mL | 1.8920 mL | 3.7840 mL | 9.4600 mL | |
| 20 mM | 0.2838 mL | 1.4190 mL | 2.8380 mL | 7.0950 mL | |
| 25 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | 5.6760 mL | |
| 30 mM | 0.1892 mL | 0.9460 mL | 1.8920 mL | 4.7300 mL | |
| 40 mM | 0.1419 mL | 0.7095 mL | 1.4190 mL | 3.5475 mL | |
| 50 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8380 mL | |
| 60 mM | 0.0946 mL | 0.4730 mL | 0.9460 mL | 2.3650 mL | |
| 80 mM | 0.0710 mL | 0.3548 mL | 0.7095 mL | 1.7738 mL | |
| 100 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL |
MK-0354 Related Classifications
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