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| Cas No.: | 1331782-27-4 |
| Chemical Name: | PF04995274,PF 04995274 |
| Synonyms: | PF04995274,PF 04995274 |
| SMILES: | OC1(CN2CCC(COC3=NOC4=C3C(O[C@H]5COCC5)=CC=C4)CC2)CCOCC1 |
| Formula: | C23H32N2O6 |
| M.Wt: | 432.22 |
| Purity: | >98% |
| Sotrage: | 4°C for 1 year, -20°C for more than 2 years |
| Description: | PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used to treat for cognitive disorders associated with Alzheimer＇s disease[1][2][3]. |
| In Vivo: | PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior[1]. Animal Model: Male 129S6/SvEv mice (7-8 weeks) treated with contextual fear conditioning (CFC) and forced swim test (FST)[1] Dosage: 3 mg/kg, 10 mg/kg Administration: Intravenous injection; for 17 days Result: Attenuated learned fear and decreased stress-induced depressive-like behavior. |
| In Vitro: | PF-04995274 has EC50 values of 0.47 nM, 0.36 nM, 0.37 nM, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively. PF-04995274 has Ki values of 0.36 nM, 0.46 nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively[3]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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