SUVN-D4010
SUVN-D4010 Basic information
- Product Name:
- SUVN-D4010
- Synonyms:
-
- SUVN-D4010
- SUVN-1004028
- SUVN-D1003019
- SUVN-D-1208045
- Usmarapride free base
- SUVN-D4010/ Usmarapride
- 1H-Indazole, 3-[5-[1-(3-methoxypropyl)-4-piperidinyl]-1,3,4-oxadiazol-2-yl]-1-(1-methylethyl)-
- CAS:
- 1428862-32-1
- MF:
- C21H29N5O2
- MW:
- 383.49
- Mol File:
- 1428862-32-1.mol
SUVN-D4010 Chemical Properties
- 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
SUVN-D4010 Usage And Synthesis
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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