Eptastigmine

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

MedKoo CAT#: 414056

CAS#: 101246-68-8

Description: Eptastigmine is a possible use in therapy of Alzheimer's disease.

Chemical Structure

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Eptastigmine
CAS# 101246-68-8
Instruction

Theoretical Analysis

MedKoo Cat#: 414056
Name: Eptastigmine
CAS#: 101246-68-8
Chemical Formula: C21H33N3O2
Exact Mass: 359.26
Molecular Weight: 359.510
Elemental Analysis: C, 70.16; H, 9.25; N, 11.69; O, 8.90

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: Eptastigmine; BRN4883778; BRN-4883778; BRN 4883778

IUPAC/Chemical Name: Carbamic acid, heptyl-, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)indol-5-yl ester, (3aS-cis)-

InChi Key: RRGMXBQMCUKRLH-FPOVZHCZSA-N

InChi Code: InChI=1S/C21H33N3O2/c1-5-6-7-8-9-13-22-20(25)26-16-10-11-18-17(15-16)21(2)12-14-23(3)19(21)24(18)4/h10-11,15,19H,5-9,12-14H2,1-4H3,(H,22,25)/t19-,21-/m0/s1

SMILES Code: O=C(OC1=CC2=C(N(C)[C@@]3([H])[C@@]2(C)CCN3C)C=C1)NCCCCCCC

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: 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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 359.51 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:
In vitro protocol:
In vivo protocol:

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1: Braida D, Sala M. Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies. CNS Drug Rev. 2001 Winter;7(4):369-86. doi: 10.1111/j.1527-3458.2001.tb00205.x. PMID: 11830755; PMCID: PMC6741646.

2: Sahoo AK, Dandapat J, Dash UC, Kanhar S. Features and outcomes of drugs for combination therapy as multi-targets strategy to combat Alzheimer's disease. J Ethnopharmacol. 2018 Apr 6;215:42-73. doi: 10.1016/j.jep.2017.12.015. Epub 2017 Dec 14. PMID: 29248451.

3: Imbimbo BP, Martelli P, Troetel WM, Lucchelli F, Lucca U, Thal LJ. Efficacy and safety of eptastigmine for the treatment of patients with Alzheimer's disease. Neurology. 1999 Mar 10;52(4):700-8. doi: 10.1212/wnl.52.4.700. PMID: 10078713.

4: Cella SG, Imbimbo BP, Pieretti F, Müller EE. Eptastigmine augments basal and GHRH-stimulated growth hormone release in young and old dogs. Life Sci. 1993;53(5):389-95. doi: 10.1016/0024-3205(93)90642-g. PMID: 8336517.

5: Mant T, Troetel WM, Imbimbo BP. Maximum tolerated dose and pharmacodynamics of eptastigmine in elderly healthy volunteers. J Clin Pharmacol. 1998 Jul;38(7):610-7. doi: 10.1002/j.1552-4604.1998.tb04467.x. PMID: 9702845.

6: Imbimbo BP, Troetel WM, Martelli P, Lucchelli F. A 6-month, double-blind, placebo-controlled trial of eptastigmine in Alzheimer's disease. Dement Geriatr Cogn Disord. 2000 Jan-Feb;11(1):17-24. doi: 10.1159/000017208. PMID: 10629357.

7: Auteri A, Mosca A, Lattuada N, Luzzana M, Zecca L, Radice D, Imbimbo BP. Pharmacodynamics and pharmacokinetics of eptastigmine in elderly subjects. Eur J Clin Pharmacol. 1993;45(4):373-6. doi: 10.1007/BF00265958. PMID: 8299673.

8: Tammenmaa-Aho I, Asher R, Soares-Weiser K, Bergman H. Cholinergic medication for antipsychotic-induced tardive dyskinesia. Cochrane Database Syst Rev. 2018 Mar 19;3(3):CD000207. doi: 10.1002/14651858.CD000207.pub2. PMID: 29553158; PMCID: PMC6494194.

9: Braida D, Ottonello F, Sala M. Eptastigmine improves eight-arm radial maze performance in aged rats. Pharmacol Res. 2000 Oct;42(4):299-304. doi: 10.1006/phrs.2000.0706. PMID: 10987987.

10: Tuovinen K, Kaliste-Korhonen E, Raushel FM, Hänninen O. Eptastigmine- phosphotriesterase combination in DFP intoxication. Toxicol Appl Pharmacol. 1996 Oct;140(2):364-9. doi: 10.1006/taap.1996.0232. PMID: 8887453.