P2Y14R antagonist 1
- CAS No.
- 2728291-29-8
- Chemical Name:
- P2Y14R antagonist 1
- Synonyms
- P2Y14R antagonist 1;Acetamide, N-1H-benzimidazol-6-yl-2-(4-bromophenoxy)-
- CBNumber:
- CB714343671
- Molecular Formula:
- C15H12BrN3O2
- Molecular Weight:
- 346.18
- MDL Number:
- MOL File:
- 2728291-29-8.mol
P2Y14R antagonist 1 Chemical Properties,Uses,Production
Uses
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[1].
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].
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 |
| 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. |
IC 50
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
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. DOI:10.1021/acs.jmedchem.4c00555
P2Y14R antagonist 1 Preparation Products And Raw materials
Raw materials
Preparation Products
P2Y14R antagonist 1 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Jinan Jiuli Biotechnology Co. , Ltd. | 15865264761 | 486064515@qq.com | China | 4771 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 25998 | 58 |
| Supplier | Advantage |
|---|---|
| Jinan Jiuli Biotechnology Co. , Ltd. | 58 |
| TargetMol Chemicals Inc. | 58 |