SHA 68_product_DataBase

Bioactivity

SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia[1][2].

Target

IC50: 22 nM (Asn107) and 23.8 nM (Ile107)

In Vivo

SHA 68 (i.p.; 5 and 50 mg/kg) reduces NPS-induced horizontal activity and vertical rearing and climbing[1]. SHA 68 (i.v.; 1 mg/kg) has a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg[1]. SHA 68 (i.p.; 2.5 mg/kg) has a T1/2 of 0.43 hours, a CL of 4.56 mL/min/kg[1]. Animal Model:

Name

SHA 68

CAS

847553-89-3

Formula

C26H24FN3O3

Molar Mass

445.49

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]. Okamura N, et al. Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor.J Pharmacol Exp The [2]. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27.

PeptideDB

SHA 68

CAS: 847553-89-3 F: C26H24FN3O3 W: 445.49