P2Y14R antagonist 1

Name: P2Y14R antagonist 1
Brand: MedChemExpress
SKU: HY-161727
Rating: 4.5 (1 reviews)

Cat. No.: HY-161727 Purity: 98.76%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC₅₀ of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis.

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

P2Y14R antagonist 1 Chemical Structure

CAS No. : 2728291-29-8

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	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y11 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

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NLRP3 NLRP1 NOD1 NOD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

P2Y14 Receptor

0.6 nM (IC₅₀)

P2Y2 Receptor

> 100 nM (IC₅₀)

P2Y6 Receptor

89.7 nM (IC₅₀)

P2Y12 Receptor

> 100 nM (IC₅₀)

P2Y1 Receptor

> 100 nM (IC₅₀)

NLRP3

In Vitro

P2Y14R antagonist 1 (compound I-17) (2-256 μM, 24 h) shows no significant cytotoxicity in RAW264.7 cells at concentrations below 256 μM^[1].
P2Y14R antagonist 1 (10-40 μM, 1 h) can counteract the effects of Uric acid sodium (HY-B2130A) and Lipopolysaccharides (HY-D1056) , demonstrating anti-gout inflammatory properties^[1].
P2Y14R antagonist 1 (10-40 μM, 1 h) acts upstream of the NLRP3 inflammasome assembly, inhibiting subsequent caspase-1 activation and macrophage pyroptosis^[1].

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

Cell Viability Assay^[1]

Cell Line:	RAW264.7 cells
Concentration:	2-256 μM
Incubation Time:	24 h
Result:	Only exhibited significant cytotoxicity only at a dose of 256 μM.

Western Blot Analysis^[1]

Cell Line:	RAW264.7 cells
Concentration:	10-40 μM
Incubation Time:	1 h
Result:	Inhibited the expression of NLRP3 and GSDMD in MSU- and LPS-treated RAW264.7 cells.

Immunofluorescence^[1]

Cell Line:	RAW264.7 cells
Concentration:	10-40 μM
Incubation Time:	1 h
Result:	Significantly reduced the formation of ASC specks induced by MSU and LPS.

In Vivo

P2Y14R antagonist 1 (compound I-17) (5-20 mg/mL, i.p., 1 h) can promote the inflammatory response caused by MSU crystal injection-induced acute gouty arthritis in the MSU-induced mouse gout model^[1].
1.19
Pharmacokinetic Analysis in MC38 Syngeneic Model^[1]

P2Y14R antagonist 1	C_max(g/mL)	T_1/2(h)	T_max (h)	AUC_0-∞(h ng/mL)	CL (L/h/kg)	F (%)
i.v. (10 mg/kg)	1533	7.6	18	1765	3.5
p.o. (30 mg/kg)	2895	12.60	32	2845	14.80	75

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

Animal Model:	Acute gouty arthritis model^[1]
Dosage:	5-20 mg/mL
Administration:	Intraperitoneal injection (i.p.) , Injection time: 60 min
Result:	Effectively reduced paw swelling in the MSU-induced mouse gout model, significantly decreased the production of pro-inflammatory cytokines IL-1β, IL-6, and IL-18 induced by MSU, markedly inhibited inflammatory cell infiltration in foot tissues induced by MSU, and significantly suppressed the increase of NLRP3 induced by MSU.

Molecular Weight

346.18

Formula

C₁₅H₁₂BrN₃O₂

CAS No.

2728291-29-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC2=C(C=C1)N=CN2)COC3=CC=C(C=C3)Br

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 : 50 mg/mL (144.43 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	2.8887 mL	14.4434 mL	28.8867 mL
5 mM	0.5777 mL	2.8887 mL	5.7773 mL
10 mM	0.2889 mL	1.4443 mL	2.8887 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 (14.44 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 (14.44 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 (14.44 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: 98.76%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (245 KB) HNMR (252 KB) LCMS (337 KB)

Handling Instructions (2659 KB)

References

[1]. Liu W, et al. Discovery of N-Substituted Acetamide Derivatives as Promising P2Y14R Antagonists Using Molecular Hybridization Based on Crystallographic Overlay. J Med Chem. 2024 Jun 27;67(12):10233-10247. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8887 mL	14.4434 mL	28.8867 mL	72.2168 mL
	5 mM	0.5777 mL	2.8887 mL	5.7773 mL	14.4434 mL
	10 mM	0.2889 mL	1.4443 mL	2.8887 mL	7.2217 mL
	15 mM	0.1926 mL	0.9629 mL	1.9258 mL	4.8145 mL
	20 mM	0.1444 mL	0.7222 mL	1.4443 mL	3.6108 mL
	25 mM	0.1155 mL	0.5777 mL	1.1555 mL	2.8887 mL
	30 mM	0.0963 mL	0.4814 mL	0.9629 mL	2.4072 mL
	40 mM	0.0722 mL	0.3611 mL	0.7222 mL	1.8054 mL
	50 mM	0.0578 mL	0.2889 mL	0.5777 mL	1.4443 mL
	60 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2036 mL
	80 mM	0.0361 mL	0.1805 mL	0.3611 mL	0.9027 mL
	100 mM	0.0289 mL	0.1444 mL	0.2889 mL	0.7222 mL