Remimazolam | CNS-7056 | CAS#308242-62-8 | CAS#1425904-79-5

MedKoo Cat#: 319813 | Name: Remimazolam

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Remimazolam, also known as CNS-7056, is a benzodiazepine derivative drug, developed by PAION, in collaboration with Japanese licensee Ono Pharmaceutical as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Remimazolam was found to be both faster acting and shorter lasting than midazolam, and human clinical trials showed a faster recovery time and predictable, consistent pharmacokinetics, suggesting some advantages over existing drugs for these applications. Remimazolam was approved in 2020

Chemical Structure

Remimazolam

CAS#308242-62-8 (freee base)

Theoretical Analysis

MedKoo Cat#: 319813

Name: Remimazolam

CAS#: 308242-62-8 (freee base)

Chemical Formula: C21H19BrN4O2

Exact Mass: 438.0691

Molecular Weight: 439.31

Elemental Analysis: C, 57.41; H, 4.36; Br, 18.19; N, 12.75; O, 7.28

Price and Availability

This product was removed for the commercial reasons.

Related CAS #

1425904-79-5 (tosylate) 308242-62-8 (freee base) 1001415-66-2 (besylate)

Synonym

CNS-7056; CNS 7056; CNS7056; Remimazolam

IUPAC/Chemical Name

methyl (S)-3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate

InChi Key

CYHWMBVXXDIZNZ-KRWDZBQOSA-N

InChi Code

InChI=1S/C21H19BrN4O2/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1

SMILES Code

O=C(OC)CC[C@H]1C2=NC=C(C)N2C3=CC=C(Br)C=C3C(C4=NC=CC=C4)=N1

Appearance

Solid powder

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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 439.31 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: Pambianco DJ, Borkett KM, Riff DS, Winkle PJ, Schwartz HI, Melson TI, Wilhelm-Ogunbiyi K. A phase IIb study comparing the safety and efficacy of remimazolam and midazolam in patients undergoing colonoscopy. Gastrointest Endosc. 2015 Sep 9. pii: S0016-5107(15)02835-7. doi: 10.1016/j.gie.2015.08.062. [Epub ahead of print] PubMed PMID: 26363333. 2: Ilic RG. Fospropofol and remimazolam. Int Anesthesiol Clin. 2015 Spring;53(2):76-90. doi: 10.1097/AIA.0000000000000053. Review. PubMed PMID: 25807020. 3: Borkett KM, Riff DS, Schwartz HI, Winkle PJ, Pambianco DJ, Lees JP, Wilhelm-Ogunbiyi K. A Phase IIa, randomized, double-blind study of remimazolam (CNS 7056) versus midazolam for sedation in upper gastrointestinal endoscopy. Anesth Analg. 2015 Apr;120(4):771-80. doi: 10.1213/ANE.0000000000000548. PubMed PMID: 25502841. 4: Zhou Y, Wang H, Jiang J, Hu P. Simultaneous determination of remimazolam and its carboxylic acid metabolite in human plasma using ultra-performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Jan 22;976-977:78-83. doi: 10.1016/j.jchromb.2014.11.022. Epub 2014 Dec 2. PubMed PMID: 25486614. 5: Goudra BG, Singh PM. Remimazolam: The future of its sedative potential. Saudi J Anaesth. 2014 Jul;8(3):388-91. doi: 10.4103/1658-354X.136627. Review. PubMed PMID: 25191193; PubMed Central PMCID: PMC4141391. 6: Worthington MT, Antonik LJ, Goldwater DR, Lees JP, Wilhelm-Ogunbiyi K, Borkett KM, Mitchell MC. A phase Ib, dose-finding study of multiple doses of remimazolam (CNS 7056) in volunteers undergoing colonoscopy. Anesth Analg. 2013 Nov;117(5):1093-100. doi: 10.1213/ANE.0b013e3182a705ae. PubMed PMID: 24108261. 7: Schnider T, Minto C. Context sensitive decrement times of remimazolam. Anesth Analg. 2013 Jul;117(1):285. doi: 10.1213/ANE.0b013e3182942954. PubMed PMID: 23788743. 8: Sneyd JR. Remimazolam: new beginnings or just a me-too? Anesth Analg. 2012 Aug;115(2):217-9. doi: 10.1213/ANE.0b013e31823acb95. PubMed PMID: 22826518. 9: Wiltshire HR, Kilpatrick GJ, Tilbrook GS, Borkett KM. A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part II. Population pharmacokinetic and pharmacodynamic modeling and simulation. Anesth Analg. 2012 Aug;115(2):284-96. doi: 10.1213/ANE.0b013e318241f68a. Epub 2012 Jan 16. PubMed PMID: 22253270. 10: Antonik LJ, Goldwater DR, Kilpatrick GJ, Tilbrook GS, Borkett KM. A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part I. Safety, efficacy, and basic pharmacokinetics. Anesth Analg. 2012 Aug;115(2):274-83. doi: 10.1213/ANE.0b013e31823f0c28. Epub 2011 Dec 20. PubMed PMID: 22190555. 11: Rogers WK, McDowell TS. Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures. IDrugs. 2010 Dec;13(12):929-37. Review. PubMed PMID: 21154153.