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847553-89-3

847553-89-3 structure
847553-89-3 structure
  • Name: SHA 68
  • Chemical Name: 3H-Oxazolo[3,4-a]pyrazine-7(1H)-carboxamide, N-[(4-fluorophenyl)methyl]tetrahydro-3-oxo-1,1-diphenyl
  • CAS Number: 847553-89-3
  • Molecular Formula: C26H24FN3O3
  • Molecular Weight: 445.48500
  • Catalog: Signaling Pathways GPCR/G Protein Neuropeptide Y Receptor
  • Create Date: 2017-06-14 02:34:04
  • Modify Date: 2025-08-20 17:59:45
  • 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].

Name 3H-Oxazolo[3,4-a]pyrazine-7(1H)-carboxamide, N-[(4-fluorophenyl)methyl]tetrahydro-3-oxo-1,1-diphenyl
Synonyms stf 083010
Description 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].
Related Catalog
Target

IC50: 22 nM (Asn107) and 23.8 nM (Ile107)[1]

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: Male C57BL/6 mice age 8-12 weeks[1] Dosage: 5 and 50 mg/kg Administration: i.p. Result: Reduced NPS-induced horizontal activity and vertical rearing and climbing. Animal Model: Male C57BL/6 mice age 8-12 weeks[1] Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: i.p. Result: Had a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg.
References

[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 Ther. 2008 Jun;325(3):893-901.

[2]. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27.

Molecular Formula C26H24FN3O3
Molecular Weight 445.48500
Exact Mass 445.18000
PSA 61.88000
LogP 4.38220
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