HCAR2 agonist 1

Name: HCAR2 agonist 1
Brand: MedChemExpress
SKU: HY-156025
Rating: 4.5 (1 reviews)

Cat. No.: HY-156025 Purity: 99.11%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

HCAR2 agonist 1 (Compound 9n) is a G_i protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the G_i protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis.

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

HCAR2 agonist 1 Chemical Structure

CAS No. : 1066676-21-8

Size	Stock	Quantity
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
25 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

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.12 μM Compound: 9n	Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 18752940]

Molecular Weight

428.53

Formula

C₂₆H₂₈N₄O₂

CAS No.

1066676-21-8

Appearance

Solid

Color

Light yellow to green yellow

SMILES

CC1=C(C(N[C@H](C)COC2=CC=CC=C2)=O)C=NC3=C(C4=CC=C(C=C4)C(C)C)C=NN13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (233.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3336 mL	11.6678 mL	23.3356 mL
5 mM	0.4667 mL	2.3336 mL	4.6671 mL
10 mM	0.2334 mL	1.1668 mL	2.3336 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 5 mg/mL (11.67 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.67 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.11%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (250 KB) HNMR (145 KB) RP-HPLC (168 KB) LCMS (384 KB)

Handling Instructions (2659 KB)

References

[1]. Zhao C, et al. Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation. Mol Cell. 2023 Sep 7;83(17):3171-3187.e7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3336 mL	11.6678 mL	23.3356 mL	58.3390 mL
	5 mM	0.4667 mL	2.3336 mL	4.6671 mL	11.6678 mL
	10 mM	0.2334 mL	1.1668 mL	2.3336 mL	5.8339 mL
	15 mM	0.1556 mL	0.7779 mL	1.5557 mL	3.8893 mL
	20 mM	0.1167 mL	0.5834 mL	1.1668 mL	2.9169 mL
	25 mM	0.0933 mL	0.4667 mL	0.9334 mL	2.3336 mL
	30 mM	0.0778 mL	0.3889 mL	0.7779 mL	1.9446 mL
	40 mM	0.0583 mL	0.2917 mL	0.5834 mL	1.4585 mL
	50 mM	0.0467 mL	0.2334 mL	0.4667 mL	1.1668 mL
	60 mM	0.0389 mL	0.1945 mL	0.3889 mL	0.9723 mL
	80 mM	0.0292 mL	0.1458 mL	0.2917 mL	0.7292 mL
	100 mM	0.0233 mL	0.1167 mL	0.2334 mL	0.5834 mL

HCAR2 agonist 1 Related Classifications

Inflammation/Immunology

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:

HCAR2 agonist 11066676-21-8Hydroxycarboxylic Acid Receptor (HCAR)anti-inflammatoryDSScolitis modelbiasedGiInhibitorinhibitorinhibit

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HCAR2 agonist 1

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HCAR2 agonist 1 Related Antibodies

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Molarity Calculator

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Complete Stock Solution Preparation Table

HCAR2 agonist 1 Related Classifications

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