Navacaprant

Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy[1].

Product Specifications

CAS Number

[2244614-14-8]

Product Name Alternative

BTRX-335140; CYM-53093

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/navacaprant.html

Purity

99.97

Solubility

1 M HCl : 3.33 mg/mL (ultrasonic) |DMSO : 3.85 mg/mL (ultrasonic; warming; adjust pH to 4 with HCl; heat to 60°C)

Smiles

CC1=NOC(C2=C(C)C3=CC(CC)=CC(F)=C3N=C2N4CCC(NC5CCOCC5)CC4)=N1

Molecular Formula

C25H32FN5O2

Molecular Weight

453.56

Precautions

H302, H315, H319

References & Citations

[1]Guerrero M, et al. Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140) . J Med Chem. 2019 Feb 28;62 (4) :1761-1780.