Usmarapride free base

SKU: orb1695133

Description

Usmarapride free base (SUVN-D4010 free base) is a selective, orally bioavailable 5-HT4 receptor partial agonist. It elevates soluble amyloid precursor protein α (sAPPα) levels and is utilized in preclinical Alzheimer's disease research, including in vitro receptor studies and in vivo cognitive function models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1428862-32-1
• MW: 383.49
• Purity: 99.91%
• Formula: C₂₁H₂₉N₅O₂
• SMILES: N=1N=C(OC1C2=NN(C=3C=CC=CC23)C(C)C)C4CCN(CCCOC)CC4
• Target: 5-HT Receptor
• Solubility: DMSO:80 mg/mL (208.61 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.61 mM)

Bioactivity

• Target IC50:
  5-HT4 receptor:44 nM (EC50)
• In Vivo:
  Methods: Usmarapride free base (1 mg/kg, oral and 1 mg/kg, intravenous) was administered to male beagle dogs to evaluate the pharmacokinetics of Usmarapride free base. Results: Usmarapride free base was rapidly absorbed after oral administration (Tmax in the range of 0.5-0.75 hours), with oral exposure (AUC0-24h = 711 ± 369 ng·h/mL) and showed a long terminal venous half-life (6.0 ± 1.5 hours), moderate venous clearance (18 ± 6 mL/min/ kg) and volume of distribution (5.1 ± 0.6 L/kg), and an absolute oral bioavailability (%F) of 72 ± 11%.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SUVN1004028, SUVN-1004028, SUVN-1004028 free base, SUVN 1004028, SUVN D 4010, SUVN D4010, SUVN D-4010, SUVN D4010 free base, SUVN-D 1003019, SUVN-D 1208045, SUVN-D 4010, SUVN-D 4010 free base, SUVN-D1003019, SUVN-D-1003019, SUVN-D1003019 free base, SUVN-D1208045, SUVN-D-1208045, SUVN-D-1208045 free base, SUVN-D4010, SUVN-D-4010, SUVN-D4010 free base, Usmarapride, Usmarapride free base

Compound Identifiers

PubChem CID

71508291