Identification | Back Directory | [Name]
SUVN-D4010 | [CAS]
1428862-32-1 | [Synonyms]
SUVN-D4010 SUVN-1004028 SUVN-D1003019 SUVN-D-1208045 Usmarapride free base SUVN-D4010/ Usmarapride | [Molecular Formula]
C21H29N5O2 | [MOL File]
1428862-32-1.mol | [Molecular Weight]
383.49 |
Chemical Properties | Back Directory | [Boiling point ]
541.9±60.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
7.84±0.10(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease[1]. | [in vivo]
Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) free base attenuates the long-term memory deficits in object recognition test (ORT)[1].
Usmarapride (1, 3, and 10 mg/kg; p.o.) free base significantly reverses the scopolamine-induced amnesia[1].
Usmarapride free base shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index[1].
Usmarapride (SUVN-D4010) free base shows good oral exposures, good bioavailability, and good brain exposures in rats[1].
| [IC 50]
5-HT4 Receptor: 44 nM (EC50) | [References]
[1] Nirogi R, et al. Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease. J Med Chem. 2021;64(15):10641-10665. DOI:10.1021/acs.jmedchem.1c00703 |
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BOC Sciences
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16314854226 |
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www.bocsci.com |
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