RS-127445 (hydrochloride)

RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites[1].

Product Specifications

CAS Number

[199864-86-3]

UNSPSC

12352005

Hazard Statement

H301, H315, H319, H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/RS-127445.html

Concentration

10mM

Purity

99.82

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

NC1=NC(C(C)C)=CC(C2=C3C=CC=CC3=C(F)C=C2)=N1.[H]Cl

Molecular Formula

C17H17ClFN3

Molecular Weight

317.79

Precautions

H301, H315, H319, H335

References & Citations

[1]Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127 (5) :1075-82.|[2]Bassil AK, et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009 Sep;158 (1) :252-8