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MedKoo Cat#: 414009 | Name: Rivastigmine free base
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Description:

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

Rivastigmine, also known as S-Rivastigmine, is an orally active and potent cholinesterase (ChE) inhibitor. Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia, particularly Alzheimer's and dementia due to Parkinson's disease.

Chemical Structure

Rivastigmine free base
Rivastigmine free base
CAS#123441-03-2 (free base)

Theoretical Analysis

MedKoo Cat#: 414009

Name: Rivastigmine free base

CAS#: 123441-03-2 (free base)

Chemical Formula: C14H22N2O2

Exact Mass: 250.1681

Molecular Weight: 250.34

Elemental Analysis: C, 67.17; H, 8.86; N, 11.19; O, 12.78

Price and Availability

Size Price Availability Quantity
1g USD 250.00 2 Weeks
5g USD 650.00 2 Weeks
10g USD 950.00 2 Weeks
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Related CAS #
123441-03-2 (free base) 129101-54-8 (tartrate)
Synonym
Rivastigmine Free Base; ENA713; ENA 713; ENA-713; S-Rivastigmine
IUPAC/Chemical Name
(S)-3-(1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
InChi Key
XSVMFMHYUFZWBK-NSHDSACASA-N
InChi Code
InChI=1S/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1
SMILES Code
O=C(OC1=CC=CC([C@@H](N(C)C)C)=C1)N(CC)C
Appearance
Liquid
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Rivastigmine inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier.
In vitro activity:
The results from this study show that rivastigmine affords neuroprotection through a mechanism that is likely unrelated to AChE inhibition. For rivastigmine, the exact mechanism is unknown. PI3K-Akt blocker 2-(4-morpholinyl)-8-phenyl-1(4H)-benzopyran-4-one hydrochloride (LY294002) did not reverse the effects of rivastigmine. Reference: J Pharmacol Exp Ther. 2005 Dec;315(3):1346-53. https://pubmed.ncbi.nlm.nih.gov/16144975/
In vivo activity:
In male rats, rivastigmine administration alleviated biochemical and histological parameters and partially ameliorated Botulinum toxin (Botox)-induced impairments. Rivastigmine could be a suitable protective approach for side effects of Botox in the hippocampus.The hippocampal cholinergic system plays a significant role in memory and learning that could be affected by Botox. Reference: Neurotoxicology. 2023 Jul 26;98:29-38. https://pubmed.ncbi.nlm.nih.gov/37507053/

Preparing Stock Solutions

The following data is based on the product molecular weight 250.34 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Terada K, Migita K, Matsushima Y, Sugimoto Y, Kamei C, Matsumoto T, Mori M, Matsunaga K, Takata J, Karube Y. Cholinesterase inhibitor rivastigmine enhances nerve growth factor-induced neurite outgrowth in PC12 cells via sigma-1 and sigma-2 receptors. PLoS One. 2018 Dec 17;13(12):e0209250. doi: 10.1371/journal.pone.0209250. PMID: 30557385; PMCID: PMC6296549. 2. Arias E, Gallego-Sandín S, Villarroya M, García AG, López MG. Unequal neuroprotection afforded by the acetylcholinesterase inhibitors galantamine, donepezil, and rivastigmine in SH-SY5Y neuroblastoma cells: role of nicotinic receptors. J Pharmacol Exp Ther. 2005 Dec;315(3):1346-53. doi: 10.1124/jpet.105.090365. Epub 2005 Sep 6. PMID: 16144975. 3. Mehri K, Oskuye ZZ, Nassireslami E, Karami E, Parvizi MR. Rivastigmine ameliorates botulinum-induced hippocampal damage and spatial memory impairment in male rats. Neurotoxicology. 2023 Jul 26;98:29-38. doi: 10.1016/j.neuro.2023.07.004. Epub ahead of print. PMID: 37507053. 4. Gupta P, Tiwari S, Singh A, Pal A, Mishra A, Singh S. Rivastigmine attenuates the Alzheimer's disease related protein degradation and apoptotic neuronal death signalling. Biochem J. 2021 Apr 16;478(7):1435-1451. doi: 10.1042/BCJ20200754. Erratum in: Biochem J. 2022 Jun 17;479(11):1147. PMID: 33660768.
In vitro protocol:
1. Terada K, Migita K, Matsushima Y, Sugimoto Y, Kamei C, Matsumoto T, Mori M, Matsunaga K, Takata J, Karube Y. Cholinesterase inhibitor rivastigmine enhances nerve growth factor-induced neurite outgrowth in PC12 cells via sigma-1 and sigma-2 receptors. PLoS One. 2018 Dec 17;13(12):e0209250. doi: 10.1371/journal.pone.0209250. PMID: 30557385; PMCID: PMC6296549. 2. Arias E, Gallego-Sandín S, Villarroya M, García AG, López MG. Unequal neuroprotection afforded by the acetylcholinesterase inhibitors galantamine, donepezil, and rivastigmine in SH-SY5Y neuroblastoma cells: role of nicotinic receptors. J Pharmacol Exp Ther. 2005 Dec;315(3):1346-53. doi: 10.1124/jpet.105.090365. Epub 2005 Sep 6. PMID: 16144975.
In vivo protocol:
1. Mehri K, Oskuye ZZ, Nassireslami E, Karami E, Parvizi MR. Rivastigmine ameliorates botulinum-induced hippocampal damage and spatial memory impairment in male rats. Neurotoxicology. 2023 Jul 26;98:29-38. doi: 10.1016/j.neuro.2023.07.004. Epub ahead of print. PMID: 37507053. 2. Gupta P, Tiwari S, Singh A, Pal A, Mishra A, Singh S. Rivastigmine attenuates the Alzheimer's disease related protein degradation and apoptotic neuronal death signalling. Biochem J. 2021 Apr 16;478(7):1435-1451. doi: 10.1042/BCJ20200754. Erratum in: Biochem J. 2022 Jun 17;479(11):1147. PMID: 33660768.
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Rivastigmine. 2020 Jan 15. PMID: 31644247. 2: Hansen RA, Gartlehner G, Webb AP, Morgan LC, Moore CG, Jonas DE. Efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer's disease: a systematic review and meta-analysis. Clin Interv Aging. 2008;3(2):211-25. PMID: 18686744; PMCID: PMC2546466. 3: Siddiqui MA, Wagstaff AJ. Rivastigmine: in Parkinson's disease dementia. CNS Drugs. 2006;20(9):739-47; discussion 748-50. doi: 10.2165/00023210-200620090-00003. PMID: 16953649. 4: Farlow MR. Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. doi: 10.1097/01.nrl.0000087724.73783.5f. PMID: 14587496. 5: Rivastigmine for Alzheimer's disease. Drug Ther Bull. 2000 Feb;38(2):15-6. PMID: 10829350. 6: Spencer CM, Noble S. Rivastigmine. A review of its use in Alzheimer's disease. Drugs Aging. 1998 Nov;13(5):391-411. doi: 10.2165/00002512-199813050-00005. PMID: 9829166. 7: Kandiah N, Pai MC, Senanarong V, Looi I, Ampil E, Park KW, Karanam AK, Christopher S. Rivastigmine: the advantages of dual inhibition of acetylcholinesterase and butyrylcholinesterase and its role in subcortical vascular dementia and Parkinson's disease dementia. Clin Interv Aging. 2017 Apr 18;12:697-707. doi: 10.2147/CIA.S129145. PMID: 28458525; PMCID: PMC5402908. 8: Grossberg GT, Sadowsky C, Olin JT. Rivastigmine transdermal system for the treatment of mild to moderate Alzheimer's disease. Int J Clin Pract. 2010 Apr;64(5):651-60. doi: 10.1111/j.1742-1241.2009.02330.x. Epub 2010 Jan 19. PMID: 20102418. 9: Maguire PA, Bastiampillai T, Allison S, Wilkes F, Looi JCL. Rivastigmine for treatment-refractory posttraumatic stress disorder: a systematic review. East Asian Arch Psychiatry. 2024 Jun;34(2):29-36. doi: 10.12809/eaap2353. PMID: 38955788. 10: Wu J, Tan Z, Pistolozzi M, Tan W. Rivastigmine-Bambuterol Hybrids as Selective Butyrylcholinesterase Inhibitors. Molecules. 2023 Dec 22;29(1):72. doi: 10.3390/molecules29010072. PMID: 38202655; PMCID: PMC10780165. 11: Birks J, Grimley Evans J, Iakovidou V, Tsolaki M. Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2000;(4):CD001191. doi: 10.1002/14651858.CD001191. Update in: Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2. PMID: 11034705. 12: Birks J, McGuinness B, Craig D. Rivastigmine for vascular cognitive impairment. Cochrane Database Syst Rev. 2013 May 31;(5):CD004744. doi: 10.1002/14651858.CD004744.pub3. PMID: 23728651. 13: Dhillon S. Rivastigmine transdermal patch: a review of its use in the management of dementia of the Alzheimer's type. Drugs. 2011 Jun 18;71(9):1209-31. doi: 10.2165/11206380-000000000-00000. PMID: 21711064. 14: Sadowsky CH, Micca JL, Grossberg GT, Velting DM. Rivastigmine from capsules to patch: therapeutic advances in the management of Alzheimer's disease and Parkinson's disease dementia. Prim Care Companion CNS Disord. 2014 Sep 4;16(5):10.4088/PCC.14r01654. doi: 10.4088/PCC.14r01654. PMID: 25667813; PMCID: PMC4321018. 15: Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE. Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2. Update in: Cochrane Database Syst Rev. 2015 Apr 10;(4):CD001191. doi: 10.1002/14651858.CD001191.pub3. PMID: 19370562. 16: Birks J, Iakovidou V, Tsolaki M. Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2000;(2):CD001191. doi: 10.1002/14651858.CD001191. Update in: Cochrane Database Syst Rev. 2000;(4):CD001191. doi: 10.1002/14651858.CD001191. PMID: 10796621. 17: Guay DR. Rivastigmine transdermal patch: role in the management of Alzheimer's disease. Consult Pharm. 2008 Aug;23(8):598-609. doi: 10.4140/tcp.n.2008.598. PMID: 19032006. 18: Monji A. [Rivastigmine]. Nihon Rinsho. 2011 Dec;69 Suppl 10 Pt 2:36-40. Japanese. PMID: 22755152. 19: Espay AJ, Marsili L, Mahajan A, Sturchio A, Pathan R, Pilotto A, Elango DS, Pezous N, Masellis M, Gomez-Mancilla B. Rivastigmine in Parkinson's Disease Dementia with Orthostatic Hypotension. Ann Neurol. 2021 Jan;89(1):91-98. doi: 10.1002/ana.25923. Epub 2020 Oct 20. PMID: 33016374. 20: Reilly S, Dhaliwal S, Arshad U, Macerollo A, Husain N, Costa AD. The effects of rivastigmine on neuropsychiatric symptoms in the early stages of Parkinson's disease: A systematic review. Eur J Neurol. 2024 Feb;31(2):e16142. doi: 10.1111/ene.16142. Epub 2023 Nov 17. PMID: 37975761; PMCID: PMC11236000.

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