P2Y14R antagonist 1
Based on 1 Customer Validation
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.
- Purity: 98.76%
- CAS No.: 2728291-29-8
- Formula: C15H12BrN3O2
- Molecular Weight:346.18
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All P2Y Receptor Isoforms
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Biological Activity
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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 |
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.
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Cell Line:RAW264.7 cells
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Concentration:2-256 μM
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Incubation Time:24 h
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Result:Only exhibited significant cytotoxicity only at a dose of 256 μM.
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Cell Line:RAW264.7 cells
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Concentration:10-40 μM
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Incubation Time:1 h
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Result:Inhibited the expression of NLRP3 and GSDMD in MSU- and LPS-treated RAW264.7 cells.
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Cell Line:RAW264.7 cells
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Concentration:10-40 μM
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Incubation Time:1 h
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Result:Significantly reduced the formation of ASC specks induced by MSU and LPS.
Pharmacokinetic Analysis in MC38 Syngeneic Model[1]
| P2Y14R antagonist 1 | Cmax(g/mL) | T1/2 (h) | Tmax (h) | AUC0-∞ (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.
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Animal Model:Acute gouty arthritis model[1]
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Dosage:5-20 mg/mL
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Administration:Intraperitoneal injection (i.p.) , Injection time: 60 min
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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.
Chemical Information
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CAS No. 2728291-29-8
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Appearance Solid
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Molecular Weight 346.18
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Formula C15H12BrN3O2
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Color White to off-white
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SMILES
O=C(NC1=CC2=C(C=C1)N=CN2)COC3=CC=C(C=C3)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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.
| 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 |
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