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P2Y14R antagonist 1

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

🥰Excellent

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

🥰Excellent

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]

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Purity:98.88%

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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
Color	White
Appearance	Solid

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

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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