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.
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- Purity : 98.76%
- CAS No.: 2728291-29-8
- 화학식: C15H12BrN3O2
- 분자량:346.18
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All P2Y Receptor Isoforms
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Biological Activity
제품 설명
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. Further protocols information, click here.
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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.
In Vivo
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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분자량 346.18
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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)
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.
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.
In Vivo Dissolution Calculator
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.
Protocol
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
순도&문서
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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 |
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| 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 |
P2Y14R antagonist 1 Related Classifications
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