MS48107_product_DataBase

Bioactivity

MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice[1].

Invitro

5-HT2B has moderate binding affinity to MS48107 (compound 71) with a Ki value of 219 nM. At 5-HT2B receptors, MS48107 shows no agonist activity but display weak antagonist activity with a Ki value of 310 nM, respectively[1].MS48107 (compound 71) has agonist activity only at the MT1 and MT2 receptors. MS48107 is a weak full agonist at the MT1 receptor (EC50 = 320 nM) and a weak partial agonist activity at the MT2 receptor (EC50 = 540 nM). MS48107 displays low binding affinities to MT1 (5900 nM) and MT2 (1100 nM) receptors[1].

In Vivo

For MS48107 (compound 71), a single intraperitoneal injection at the dose of 25 mg/kg leads to high exposure levels (above 10 μM) in both plasma and brain at 0.5 h in mice (Swiss Albino mice). The high compound exposure levels in both plasma and brain are maintained for 2 h[1].

Name

MS48107

CAS

2375070-79-2

Formula

C23H20FN5O2

Molar Mass

417.44

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Xufen Yu, et al. Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). J Med Chem. 2019 Aug 22;62(16):7557-7574.

PeptideDB

MS48107

CAS: 2375070-79-2 F: C23H20FN5O2 W: 417.44