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P2Y14R antagonist 1

Name: P2Y14R antagonist 1
Brand: TargetMol
SKU: T88677
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T88677Cas No. 2728291-29-8

P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis.

P2Y14R antagonist 1

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Purity: 98.88%

Catalog No. T88677Cas No. 2728291-29-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$42	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$156	In Stock	In Stock
25 mg	$313	In Stock	In Stock
50 mg	$493	In Stock	In Stock
100 mg	$786	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.88%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis.
Targets&IC50	P2Y14 receptor (HEK293 cells):0.11 nM (Kᴅ), P2Y14 receptor (HEK293 cells):0.60 nM
In vitro	P2Y14R antagonist 1 （Compound I-17）showed potent inhibition of P2Y14R in HEK293 cells (IC₅₀ = 0.60 nM; K_D = 0.11 nM) and had no significant effect on other P2Y receptors[1]. In RAW264.7 cells, P2Y14R antagonist 1 (10–40 μM) inhibited MSU+LPS-induced IL-1β, IL-6, and IL-18 release, reduced NLRP3 and GSDMD expression, and suppressed pyroptosis[1].
In vivo	P2Y14R antagonist 1（compound I-17）exhibited good oral bioavailability (F = 75%) in rats (20 mg/kg, p.o., T₁/₂ = 12.6 h). In an MSU-induced mouse model of acute gouty arthritis, P2Y14R antagonist 1 effectively reduced paw swelling, downregulated pro-inflammatory cytokines (IL-1β, IL-6, IL-18), attenuated immune cell infiltration and joint histopathological damage, and decreased NLRP3 expression[1].

Chemical Properties

Molecular Weight	346.18
Formula	C₁₅H₁₂BrN₃O₂
Cas No.	2728291-29-8
Smiles	O=C(NC=1C=CC=2N=CNC2C1)COC3=CC=C(Br)C=C3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (115.55 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8887 mL	14.4434 mL	28.8867 mL	144.4335 mL
5 mM	0.5777 mL	2.8887 mL	5.7773 mL	28.8867 mL
10 mM	0.2889 mL	1.4443 mL	2.8887 mL	14.4434 mL
20 mM	0.1444 mL	0.7222 mL	1.4443 mL	7.2217 mL
50 mM	0.0578 mL	0.2889 mL	0.5777 mL	2.8887 mL
100 mM	0.0289 mL	0.1444 mL	0.2889 mL	1.4443 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc