Synonym
Zaltoprofen; CN-100; CN100; CN 100
IUPAC/Chemical Name
2-(10-oxo-10,11-dihydrodibenzo[b,f]thiepin-2-yl)propanoic acid
InChi Key
MUXFZBHBYYYLTH-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20)
SMILES Code
CC(C1=CC=C(C(C2)=C1)SC3=CC=CC=C3C2=O)C(O)=O
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).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
298.36
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: Jia L, Hu C, Wang H, Liu Y, Liu X, Zhang YY, Li W, Wang LX, Cao YF, Fang ZZ. Chirality Influence of Zaltoprofen Towards UDP-Glucuronosyltransferases (UGTs) Inhibition Potential. Chirality. 2015 Jun;27(6):359-63. doi: 10.1002/chir.22436. Epub 2015 Apr 22. PubMed PMID: 25903196.
2: Mishra R, Prabhavalkar KS, Bhatt LK. Preparation, optimization, and evaluation of Zaltoprofen-loaded microemulsion and microemulsion-based gel for transdermal delivery. J Liposome Res. 2016 Dec;26(4):297-306. doi: 10.3109/08982104.2015.1120746. Epub 2016 Jan 19. PubMed PMID: 26785055.
3: Cui H, Quan P, Zhao H, Wen X, Song W, Xiao Y, Zhao Y, Fang L. Mechanism of Ion-Pair Strategy in Modulating Skin Permeability of Zaltoprofen: Insight from Molecular-Level Resolution Based on Molecular Modeling and Confocal Laser Scanning Microscopy. J Pharm Sci. 2015 Oct;104(10):3395-403. doi: 10.1002/jps.24543. Epub 2015 Jun 17. PubMed PMID: 26349639.
4: Baek JS, Lim JH, Kang JS, Shin SC, Jung SH, Cho CW. Enhanced transdermal drug delivery of zaltoprofen using a novel formulation. Int J Pharm. 2013 Sep 10;453(2):358-62. doi: 10.1016/j.ijpharm.2013.05.059. Epub 2013 Jun 4. PubMed PMID: 23747435.
5: Cho IJ, Lee CW, Lee MY, Kang MR, Yun J, Oh SJ, Han SB, Lee K, Park SK, Kim HM, Jung SH, Kang JS. Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents. Int Immunopharmacol. 2013 Aug;16(4):457-60. doi: 10.1016/j.intimp.2013.05.008. Epub 2013 May 27. PubMed PMID: 23721690.
6: Cui H, Quan P, Zhou Z, Fang L. Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation. Drug Deliv. 2016 Jul 16:1-10. [Epub ahead of print] PubMed PMID: 27257038.
7: Pawar S, Pande V. Oleic Acid Coated Gelatin Nanoparticles Impregnated Gel for Sustained Delivery of Zaltoprofen: Formulation and Textural Characterization. Adv Pharm Bull. 2015 Nov;5(4):537-48. doi: 10.15171/apb.2015.073. Epub 2015 Nov 30. PubMed PMID: 26819927; PubMed Central PMCID: PMC4729344.
8: Shah HA, Patel RP. Statistical modeling of zaltoprofen loaded biopolymeric nanoparticles: Characterization and anti-inflammatory activity of nanoparticles loaded gel. Int J Pharm Investig. 2015 Jan-Mar;5(1):20-7. doi: 10.4103/2230-973X.147229. PubMed PMID: 25599029; PubMed Central PMCID: PMC4286831.
9: Wang H, Ji J, Zeng S. Biosynthesis and stereoselective analysis of (-)- and (+)-zaltoprofen glucuronide in rat hepatic microsomes and its application to the kinetic analysis. J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Aug 15;879(24):2430-6. doi: 10.1016/j.jchromb.2011.06.043. Epub 2011 Jul 6. PubMed PMID: 21775222.
10: Kohno T. Zaltoprofen inhibits bradykinin-mediated enhancement of glutamate receptor activity in substantia gelatinosa neurons. Anesth Analg. 2011 Aug;113(2):412-6. doi: 10.1213/ANE.0b013e31821c693c. Epub 2011 Apr 25. PubMed PMID: 21519044.
