MK-0354

Name: MK-0354
Brand: MedChemExpress
SKU: HY-13008
Rating: 4.5 (1 reviews)

Cat. No.: HY-13008 Purity: 99.73%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

MK-0354 Chemical Structure

CAS No. : 851776-28-8

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE MK-0354

•Nat Commun. 2023 Mar 27;14(1):1710. [Abstract]

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Biological Activity
Purity & Documentation
References
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Description

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^[1]^[2]^[3]^[4].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.286 μM Compound: MK-0354	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	[PMID: 20363624]
CHO	EC₅₀	286 nM Compound: 1, MK-0354	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	[PMID: 22435740]

In Vitro

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.

In Vivo

MK-0354 (50 mg/kg; i.p.; daily; 7 days before tumor implantation and continued until the end of the experiment) fails to suppress tumor growth or alter immune cell infiltration in Hepa1-6 tumor-bearing C57BL/6 mice^[4].

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

Clinical Trial

Molecular Weight

176.18

Formula

C₇H₈N₆

CAS No.

851776-28-8

Appearance

Solid

Color

Light yellow to khaki

SMILES

C12=C(CCC2)C(C3=NN=NN3)=NN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.6760 mL	28.3801 mL	56.7601 mL
5 mM	1.1352 mL	5.6760 mL	11.3520 mL
10 mM	0.5676 mL	2.8380 mL	5.6760 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (251 KB) HNMR (139 KB) RP-HPLC (163 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

References

[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

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

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:

MK-0354851776-28-8MK0354MK 0354GPR109AHM74APUMA-GHCA2HCAR2 Inhibitorinhibitorinhibit

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MK-0354

Customer Review

MK-0354 Related Antibodies

1 Publications Citing Use of MCE MK-0354

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

MK-0354 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

MK-0354 Related Classifications

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