Synonym
SCH-486757; SCH486757; SCH 486757
IUPAC/Chemical Name
8-Azabicyclo(3.2.1)octan-3-ol, 8-(bis(2-chlorophenyl)methyl)-3-(2-pyrimidinyl)-
SMILES Code
ClC1=CC=CC=C1C(N2[C@@H]3CC[C@H]2C[C@](C4=NC=CC=N4)(O)C3)C5=CC=CC=C5Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Preparing Stock Solutions
The following data is based on the
product
molecular weight
440.37
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: McLeod RL, Tulshian DB, Bolser DC, Varty GB, Baptista M, Fernandez X, Parra LE, Zimmer JC, Erickson CH, Ho GD, Jia Y, Ng FW, Korfmacher W, Xu X, Veals J, Smith-Torhan A, Wainhaus S, Fawzi AB, Austin TM, van Heek M, Hey JA. Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models. Eur J Pharmacol. 2010 Mar 25;630(1-3):112-20. doi: 10.1016/j.ejphar.2009.12.003. PubMed PMID: 20006596; PubMed Central PMCID: PMC2922759.
2: Enright BP, McIntyre BS, Barat SA, Treinen KA, Kopytek SJ. Effects of SCH 486757, a nociceptin-1 receptor agonist, on fertility and reproductive hormone levels in female CRL:CD®[SD] rats. Birth Defects Res B Dev Reprod Toxicol. 2012 Feb;95(1):12-22. doi: 10.1002/bdrb.20334. PubMed PMID: 21922640.
3: Penner NA, Ho G, Bercovici A, Chowdhury SK, Alton KB. Identification of two novel metabolites of SCH 486757, a nociceptin/orphanin FQ peptide receptor agonist, in humans. Drug Metab Dispos. 2010 Nov;38(11):2067-74. doi: 10.1124/dmd.110.032516. PubMed PMID: 20671096.
4: McLeod RL, Tulshian DB, Sadeh J. Where are the new cough treatments: a debriefing of recent clinical proof-of-concept trials with the NOP agonist SCH 486757. Pharmacology. 2011;88(1-2):50-4. doi: 10.1159/000328782. Review. PubMed PMID: 21757975.
5: Spina D, Page CP. Regulating cough through modulation of sensory nerve function in the airways. Pulm Pharmacol Ther. 2013 Oct;26(5):486-90. doi: 10.1016/j.pupt.2013.03.011. PubMed PMID: 23524012.
6: Woodcock A, McLeod RL, Sadeh J, Smith JA. The efficacy of a NOP1 agonist (SCH486757) in subacute cough. Lung. 2010 Jan;188 Suppl 1:S47-52. doi: 10.1007/s00408-009-9197-8. PubMed PMID: 19937046.
