Synonym
CS386; CS-386; CS 386; Melex; Sedoxil; Mexazolam
IUPAC/Chemical Name
10-chloro-11b-(2-chlorophenyl)-3-methyl-2,3,7,11b-tetrahydrobenzo[f]oxazolo[3,2-d][1,4]diazepin-6(5H)-one
InChi Key
ANUCDXCTICZJRH-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H16Cl2N2O2/c1-11-10-24-18(13-4-2-3-5-15(13)20)14-8-12(19)6-7-16(14)21-17(23)9-22(11)18/h2-8,11H,9-10H2,1H3,(H,21,23)
SMILES Code
O=C1NC2=CC=C(Cl)C=C2C(OCC3C)(C4=CC=CC=C4Cl)N3C1
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, not in water
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
363.24
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: Fernandes H, Moreira R. Mexazolam: clinical efficacy and tolerability in the treatment of anxiety. Neurol Ther. 2014 Mar 29;3(1):1-14. doi: 10.1007/s40120-014-0016-7. eCollection 2014 Jun. Review. PubMed PMID: 26000220; PubMed Central PMCID: PMC4381915.
2: Weon Cho C, Chul Shin S. Enhanced Controlled Transdermal Delivery of Mexazolam Using Ethylene-vinyl Acetate. Iran J Pharm Res. 2012 Winter;11(1):3-12. PubMed PMID: 25317180; PubMed Central PMCID: PMC3876569.
3: Ferreira L, Figueira ML, Bessa-Peixoto A, Marieiro A, Albuquerque R, Paz C, Cerqueira A, Damião P, Dolgner A, Dingemanse J. Psychomotor and anxiolytic effects of mexazolam in patients with generalised anxiety disorder. Clin Drug Investig. 2003;23(4):235-43. PubMed PMID: 17535036.
4: Ishigami M, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y. Sex difference in inhibition of in vitro mexazolam metabolism by various 3-hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors in rat liver microsomes. Drug Metab Dispos. 2002 Aug;30(8):904-10. PubMed PMID: 12124308.
5: Ishigami M, Honda T, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y. A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. Drug Metab Dispos. 2001 Mar;29(3):282-8. PubMed PMID: 11181496.
6: Kurono Y, Kamiya K, Kuwayama T, Jinno Y, Yashiro T, Ikeda K. Kinetics and mechanism of the acid-base equilibrium of mexazolam and comparison with those of other commercial benzodiazepinooxazole drugs. Chem Pharm Bull (Tokyo). 1987 Sep;35(9):3831-7. PubMed PMID: 2893667.