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| Cas No.: | 847553-89-3 |
| Chemical Name: | SHA 68 |
| Synonyms: | SHA 68;3-Oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide;N-[(4-Fluorophenyl)methyl]tetrahydro-3-oxo-1,1-diphenyl-3H-oxazolo[3,4-a]pyrazine-7(1H)-carboxamide;SHA-68;N-[(4-Fluorophenyl)methyl]tetrahydro-3-oxo-1,1-diphenyl-3H-oxazolo[3,4-a]pyrazine-7(1H)-carboxamide (ACI) |
| SMILES: | O=C1N2CCN(CC2C(C2C=CC=CC=2)(C2C=CC=CC=2)O1)C(NCC1C=CC(F)=CC=1)=O |
| Formula: | C26H24FN3O3 |
| M.Wt: | 445.485469818115 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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]. |
| 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. |
MSDS
| TITLE | DOWNLOAD |
| MSDS_12298_DC28243_847553-89-3 |
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