Synonym
ASP-8477; ASP8477; ASP 8477;
IUPAC/Chemical Name
pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate
InChi Key
PLCMZPFTMOAGOE-UHFFFAOYSA-N
InChi Code
1S/C18H19N3O3/c22-17(20-15-5-2-1-3-6-15)14-8-11-21(12-9-14)18(23)24-16-7-4-10-19-13-16/h1-7,10,13-14H,8-9,11-12H2,(H,20,22)
SMILES Code
O=C(NC1=CC=CC=C1)C2CCN(CC2)C(=O)OC3=CN=CC=C3
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
325.37
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: Kiso T, Watabiki T, Sekizawa T. ASP8477, a fatty acid amide hydrolase inhibitor, exerts analgesic effects in rat models of neuropathic and dysfunctional pain. Eur J Pharmacol. 2020 Aug 15;881:173194. doi: 10.1016/j.ejphar.2020.173194. Epub 2020 May 21. PMID: 32445705.
2: Treijtel N, Collins C, van Bruijnsvoort M, Fuhr R, Ernault E, Gangaram-Panday S, Passier P. A Cocktail Interaction Study Evaluating the Drug-Drug Interaction Potential of the Perpetrator Drug ASP8477 at Multiple Ascending Dose Levels. Clin Pharmacol Drug Dev. 2019 May;8(4):529-540. doi: 10.1002/cpdd.660. Epub 2019 Feb 7. PMID: 30730615; PMCID: PMC6593727.
3: Schaffler K, Yassen A, Reeh P, Passier P. A Randomized, Double-Blind, Placebo- and Active Comparator-Controlled Phase I Study of Analgesic/Antihyperalgesic Properties of ASP8477, a Fatty Acid Amide Hydrolase Inhibitor, in Healthy Female Subjects. Pain Med. 2018 Jun 1;19(6):1206-1218. doi: 10.1093/pm/pnx281. PMID: 29228247; PMCID: PMC5998989.
4: Watabiki T, Tsuji N, Kiso T, Ozawa T, Narazaki F, Kakimoto S. In vitro and in vivo pharmacological characterization of ASP8477: A novel highly selective fatty acid amide hydrolase inhibitor. Eur J Pharmacol. 2017 Nov 15;815:42-48. doi: 10.1016/j.ejphar.2017.10.007. Epub 2017 Oct 7. PMID: 29017758.
5: Bradford D, Stirling A, Ernault E, Liosatos M, Tracy K, Moseley J, Blahunka P, Smith MD. The MOBILE Study-A Phase IIa Enriched Enrollment Randomized Withdrawal Trial to Assess the Analgesic Efficacy and Safety of ASP8477, a Fatty Acid Amide Hydrolase Inhibitor, in Patients with Peripheral Neuropathic Pain. Pain Med. 2017 Dec 1;18(12):2388-2400. doi: 10.1093/pm/pnx046. PMID: 28383710; PMCID: PMC5939857.
