Rivastigmine Tartrate
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MedKoo CAT#: 318672

CAS#: 129101-54-8 (tartrate)

Description: Rivastigmine tartrate is an orally active and potent cholinesterase (ChE) inhibitor. Rivastigmine tartrate 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

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Rivastigmine Tartrate
CAS# 129101-54-8 (tartrate)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 318672
Name: Rivastigmine Tartrate
CAS#: 129101-54-8 (tartrate)
Chemical Formula: C18H28N2O8
Exact Mass: 0.00
Molecular Weight: 400.420
Elemental Analysis: C, 53.99; H, 7.05; N, 7.00; O, 31.96

Price and Availability

Size Price Availability Quantity
200mg USD 250
500mg USD 450
1g USD 650
2g USD 950
5g USD 1650
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Related CAS #: 123441-03-2 (free base)   129101-54-8 (tartrate)  

Synonym: ENA713; ENA 713; ENA-713; SDZ-ENA 713; SDZ-ENA713; SDZ-ENA-713; Rivastigmine Tartrate; Rivastigmine bitartrate.

IUPAC/Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid;[3-[(1S)-1-(dimethylamino)ethyl]phenyl] N-ethyl-N-methylcarbamate

InChi Key: GWHQHAUAXRMMOT-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H22N2O2.C4H6O6/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4;5-1(3(7)8)2(6)4(9)10/h7-11H,6H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)

SMILES Code: CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C.C(C(C(=O)O)O)(C(=O)O)O

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 water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in water

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:
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Biological target: Rivastigmine tartrate inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate 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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 50.0 124.87

Preparing Stock Solutions

The following data is based on the product molecular weight 400.42 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.

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1: Spiridigliozzi GA, Hart SJ, Heller JH, Schneider HE, Baker JA, Weadon C,
Capone GT, Kishnani PS. Safety and efficacy of rivastigmine in children with Down
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2: Nieto RA, Deardorff WJ, Grossberg GT. Efficacy of rivastigmine tartrate,
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3: Mohamed LA, Keller JN, Kaddoumi A. Role of P-glycoprotein in mediating
rivastigmine effect on amyloid-β brain load and related pathology in Alzheimer's
disease mouse model. Biochim Biophys Acta. 2016 Apr;1862(4):778-87. doi:
10.1016/j.bbadis.2016.01.013. Epub 2016 Jan 15. PubMed PMID: 26780497; PubMed
Central PMCID: PMC4788561.


4: Papp M, Gruca P, Lason-Tyburkiewicz M, Willner P. Antidepressant, anxiolytic
and procognitive effects of rivastigmine and donepezil in the chronic mild stress
model in rats. Psychopharmacology (Berl). 2016 Apr;233(7):1235-43. doi:
10.1007/s00213-016-4206-0. Epub 2016 Jan 15. PubMed PMID: 26769042; PubMed
Central PMCID: PMC4801996.


5: Zhang ZX, Hong Z, Wang YP, He L, Wang N, Zhao ZX, Zhao G, Shang L, Weisskopf
M, Callegari F, Strohmaier C. Rivastigmine Patch in Chinese Patients with
Probable Alzheimer's disease: A 24-week, Randomized, Double-Blind Parallel-Group
Study Comparing Rivastigmine Patch (9.5 mg/24 h) with Capsule (6 mg Twice Daily).
CNS Neurosci Ther. 2016 Mar 25. doi: 10.1111/cns.12521. [Epub ahead of print]
PubMed PMID: 27012596.


6: Bokde AL, Cavedo E, Lopez-Bayo P, Lista S, Meindl T, Born C, Galluzzi S,
Faltraco F, Dubois B, Teipel SJ, Reiser M, Möller HJ, Hampel H. Effects of
rivastigmine on visual attention in subjects with amnestic mild cognitive
impairment: A serial functional MRI activation pilot-study. Psychiatry Res. 2016
Mar 30;249:84-90. doi: 10.1016/j.pscychresns.2016.01.018. Epub 2016 Jan 18.
PubMed PMID: 26851974.


7: Simon A, Amaro MI, Cabral LM, Healy AM, de Sousa VP. Development of a novel
dry powder inhalation formulation for the delivery of rivastigmine hydrogen
tartrate. Int J Pharm. 2016 Mar 30;501(1-2):124-38. doi:
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8: Henderson EJ, Lord SR, Brodie MA, Gaunt DM, Lawrence AD, Close JC, Whone AL,
Ben-Shlomo Y. Rivastigmine for gait stability in patients with Parkinson's
disease (ReSPonD): a randomised, double-blind, placebo-controlled, phase 2 trial.
Lancet Neurol. 2016 Mar;15(3):249-58. doi: 10.1016/S1474-4422(15)00389-0. Epub
2016 Jan 13. PubMed PMID: 26795874.


9: Higashino K, Ago Y, Umeki T, Hasebe S, Onaka Y, Hashimoto H, Takuma K, Matsuda
T. Rivastigmine improves isolation rearing-induced prepulse inhibition deficits
via muscarinic acetylcholine receptors in mice. Psychopharmacology (Berl). 2016
Feb;233(3):521-8. doi: 10.1007/s00213-015-4123-7. Epub 2015 Oct 31. PubMed PMID:
26518025.


10: Imbernón-Moya A, Podlipnik S, Burgos F, Vargas-Laguna E, Aguilar-Martínez A,
Fernández-Cogolludo E, Gallego-Valdes MA. Acquired Localized Hypertrichosis
Induced by Rivastigmine. Case Rep Dermatol Med. 2016;2016:7296572. doi:
10.1155/2016/7296572. Epub 2016 Mar 17. PubMed PMID: 27073702; PubMed Central
PMCID: PMC4814665.


11: Bezerra da Silva C, Pott A, Elifio-Esposito S, Dalarmi L, Fialho do
Nascimento K, Moura Burci L, de Oliveira M, de Fátima Gaspari Dias J, Maria
Warumby Zanin S, Gomes Miguel O, Dallarmi Miguel M. Effect of Donepezil, Tacrine,
Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia
tigrina. Molecules. 2016 Jan 11;21(1). pii: E53. doi: 10.3390/molecules21010053.
PubMed PMID: 26760993.


12: Soysal P, Isik AT. Asymptomatic Bradycardia Due to Rivastigmine in an Elderly
Adult with Lewy Body Dementia. J Am Geriatr Soc. 2015 Dec;63(12):2648-2650. doi:
10.1111/jgs.13858. PubMed PMID: 26691714.


13: Shah B, Khunt D, Bhatt H, Misra M, Padh H. Application of quality by design
approach for intranasal delivery of rivastigmine loaded solid lipid
nanoparticles: Effect on formulation and characterization parameters. Eur J Pharm
Sci. 2015 Oct 12;78:54-66. doi: 10.1016/j.ejps.2015.07.002. Epub 2015 Jul 2.
PubMed PMID: 26143262.


14: van Schaik AM, Rhebergen D, Henstra MJ, Kadouch DJ, van Exel E, Stek ML.
Cognitive Impairment and Electroconvulsive Therapy in Geriatric Depression, What
Could be the Role of Rivastigmine? A Case Series. Clin Pract. 2015 Sep
28;5(3):780. doi: 10.4081/cp.2015.780. eCollection 2015 Sep 28. PubMed PMID:
26664715; PubMed Central PMCID: PMC4653751.


15: Nakamura Y, Strohmaier C, Tamura K, Kataoka N, Nakano M, Oda S, Nishimura K,
Homma A. A 24-Week, Randomized, Controlled Study to Evaluate the Tolerability,
Safety and Efficacy of 2 Different Titration Schemes of the Rivastigmine Patch in
Japanese Patients with Mild to Moderate Alzheimer's Disease. Dement Geriatr Cogn
Dis Extra. 2015 Sep 29;5(3):361-74. doi: 10.1159/000439269. eCollection 2015
Sep-Dec. PubMed PMID: 26557135; PubMed Central PMCID: PMC4637522.


16: Birks JS, Chong LY, Grimley Evans J. Rivastigmine for Alzheimer's disease.
Cochrane Database Syst Rev. 2015 Sep 22;9:CD001191. [Epub ahead of print] Review.
PubMed PMID: 26393402.


17: Isaacson RS, Ferris S, Velting DM, Meng X. Cognitive Efficacy (SIB) of 13.3
Versus 4.6 mg/24 h Rivastigmine Patch in Severe Alzheimer's Disease. Am J
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18: D'Onofrio G, Sancarlo D, Addante F, Ciccone F, Cascavilla L, Paris F, Elia
AC, Nuzzaci C, Picoco M, Greco A, Panza F, Pilotto A. A pilot randomized
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patch and cognitive stimulation in patients with Alzheimer's disease. Int J
Geriatr Psychiatry. 2015 Sep;30(9):965-75. doi: 10.1002/gps.4247. Epub 2014 Dec
12. PubMed PMID: 25504466.


19: Diaz MC, Rosales RL. A Case Report on Dyskinesia Following Rivastigmine Patch
13.3 mg/24 hours for Alzheimer's Disease: Perspective in the Movement Disorders
Spectrum Following Use of Cholinesterase Inhibitors. Medicine (Baltimore). 2015
Aug;94(34):e1364. doi: 10.1097/MD.0000000000001364. PubMed PMID: 26313774; PubMed
Central PMCID: PMC4602930.


20: Zamani M, Mohammadi M, Zamani H, Tavasoli A. Pharmacogenetic Study on the
Impact of Rivastigmine Concerning Genetic Variants of A2M and IL-6 Genes on
Iranian Alzheimer's Patients. Mol Neurobiol. 2015 Aug 21. [Epub ahead of print]
PubMed PMID: 26289409.