[CAS NO. 1428862-33-2] Usmarapride
PRODUCTS SPECIFICATIONS [1428862-33-2]
DESCRIPTION [1428862-33-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 473.52 |
| Molecular Formula | C23H31N5O6 |
| SMILES | CC(N1N=C(C2=NN=C(C3CCN(CCCOC)CC3)O2)C4=C1C=CC=C4)C.O=C(O)C(O)=O |
Summary
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT 4 receptor partial agonist ( EC 50 =44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease [1] .
IC50 & Target
|
5-HT 4 Receptor 44 nM (EC 50 ) |
In Vivo
Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) attenuates the long-term memory deficits in object recognition test (ORT)
[1]
.
Usmarapride (1, 3, and 10 mg/kg; p.o.) significantly reverses the scopolamine-induced amnesia
[1]
.
Usmarapride shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index
[1]
.
Usmarapride (SUVN-D4010) shows good oral exposures, good bioavailability, and good brain exposures in rats
[1]
.
Pharmacokinetic of Usmarapride in Rats
[1]
(3.0 mg/kg for p.o. dosing; 1.0 mg/kg for i.v.)
| F% | C max (ng/mL) | AUC (ng·hr/mL) | t 1/2 (h) | V dss (L/kg) | CL (mLg/min/kg) |
| 34 | 360 | 709 | 1.7 | 8.0 | 76 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02575482 | Suven Life Sciences Limited |
Cognitive Disorders
|
July 2015 | Phase 1 |
| NCT03031574 | Suven Life Sciences Limited |
Cognitive Disorder
|
January 23, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 33.33 mg/mL ( 70.39 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1118 mL | 10.5592 mL | 21.1184 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2237 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL |