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CTEP
产品别名
871362-31-1
CTEP
2-CHLORO-4-((2,5-DIMETHYL-1-(4-(TRIFLUOROMETHOXY)PHENYL)-1H-IMIDAZOL-4-YL)ETHYNYL)PYRIDINE
RO4956371
2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C19H13ClF3N3O |
| Molecular weight | 391.77 |
| MDL number | MFCD22665726 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | CTEP is a high-affinity, orally active, potent and selective metabotropic glutamate receptor 5 (mGlu5 or mGluR5) negative allosteric modulator (NAM) and inverse agonist (human/mouse/rat mGlu5 Kd = 1.7/1.8/1.5 nM; IC50 against quisqualate stimulation = 6.4/16.8/8/8 by IP accumulation or 11.4/42/4/6.9 by Ca2+ mobilization using human/mouse/rat mGlu5 HEK293 transfectants; IC50 = 40.1 nM against constitutive IP level in human mGlu5 HEK293) with >1000-fold selectivity over 103 molecular targets, including all known mGluRs. CTEP is an excellent tool compound for long-term in vivo studies (in mice and rats) with good pharmacokinetic properties (B/P ratio = 2.6, oral bioavailability ~100%, T1/2 ~18 hrs post 4.5 mg/kg p.o. in mice) and reported to display 30- to 100-fold higher in vivo potency than MPEP and fenobam in two rodent behavioral models sensitive to antianxiety drugs. CTEP (RO4956371) may be used as a therapeutic to reduce hippocampal long-term depression, protein synthesis, and audiogenic seizures in the fragile X mental retardation 1 (Fmr1) knockout mouse. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CC1=C(C#CC2=CC(Cl)=NC=C2)N=C(C)N1C3=CC=C(OC(F)(F)F)C=C3 |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
