PF-04995274
Modify Date: 2024-01-11 17:43:44
PF-04995274 structure
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Common Name | PF-04995274 | ||
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| CAS Number | 1331782-27-4 | Molecular Weight | 432.51000 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H32N2O6 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of PF-04995274PF-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]. |
| Name | 4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| Target |
5-HT4 receptor[1][2][3] |
| 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]. |
| 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. |
| References |
| Molecular Formula | C23H32N2O6 |
|---|---|
| Molecular Weight | 432.51000 |
| Exact Mass | 432.22600 |
| PSA | 86.42000 |
| LogP | 2.56570 |
| RIDADR | NONH for all modes of transport |
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| unii-xi179pg9lv |
| PF-04995274 |