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YJC-10592
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C27H31ClF3N5O3
- MW: 566.01
Description
YJC-10592 is a CC chemokine receptor 2 (CCR2) antagonist with a biochemical binding IC50 value of 1.12 μM. Despite this moderate baseline affinity, it exhibits exceptional functional potency, inhibiting calcium mobilization at an IC50 of 1.7 nM and cell chemotaxis assays at 23 nM. In rats in vivo studies, YJC-10592 displayed dose-dependent pharmacokinetics alongside low oral bioavailability.
CCR2 pharmacology is highly applicable to translational and disease-specific cell models. YJC-10592 serves as a valuable tool compound, supporting mechanistic studies of CCR2 pathways across biochemical, cellular, and phenotypic disease assays.
Key Features
- CCR2 antagonist for interrogation of CCR2 biology
- Exhibits exceptional functional potency
- Modulates CCR2-dependent signaling or biological activity
- Displays dose-dependent pharmacokinetics
Applications
- CCR2 pharmacology and target-validation studies
- CCR2 pathway and signaling assays
- Disease-relevant cellular and translational model systems
- Receptor signaling, ligand profiling and functional response assays
More Information
| Parent CAS No. | 1226894-87-6 |
|---|---|
| Chemical Name | (R)-N-(2-(1-(2-(4-(2-chlorobenzoyl)piperazin-1-yl)ethyl)pyrrolidin-3-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide |
| SMILES | C1(C(=O)NCC(=O)N[C@@H]2CCN(CCN3CCN(C(C4C(Cl)=CC=CC=4)=O)CC3)C2)C=C(C(F)(F)F)C=CC=1 |&1:8,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H31ClF3N5O3/c28-23-7-2-1-6-22(23)26(39)36-14-12-34(13-15-36)10-11-35-9-8-21(18-35)33-24(37)17-32-25(38)19-4-3-5-20(16-19)27(29,30)31/h1-7,16,21H,8-15,17-18H2,(H,32,38)(H,33,37)/t21-/m1/s1 |
| InChiKey | HTXMSBSZASVVFP-OAQYLSRUSA-N |
| CID | 46830335 |
| Short Description | CCR2 antagonist |
References
- JW Lim et al. Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2099-102.
- ES Du et al. Pharmacokinetics of YJC-10592, a novel chemokine receptor 2 (CCR-2) antagonist, in rats. Arch Pharm Res. 2016 Jun;39(6):833-42.
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