847553-89-3
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: 2024-01-03 18:32:44
-
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 |
| Molecular Formula | C26H24FN3O3 |
|---|---|
| Molecular Weight | 445.48500 |
| Exact Mass | 445.18000 |
| PSA | 61.88000 |
| LogP | 4.38220 |