Samidorphan

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

MedKoo CAT#: 461748

CAS#: 852626-89-2

Description: Samidorphan, also known as ALKS-33 and RDC-0313, is an opioid modulator with μ-antagonist properties. It is under development by Alkermes for the treatment of major depressive disorder and possibly other psychiatric conditions.


Chemical Structure

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Samidorphan
CAS# 852626-89-2

Theoretical Analysis

MedKoo Cat#: 461748
Name: Samidorphan
CAS#: 852626-89-2
Chemical Formula: C21H26N2O4
Exact Mass: 370.1893
Molecular Weight: 370.44
Elemental Analysis: C, 68.09; H, 7.07; N, 7.56; O, 17.28

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.

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Synonym: Samidorphan; RDC 0313; RDC-0313; RDC0313; ALKS-33; ALKS33; ALKS 33;

IUPAC/Chemical Name: (4bR,8aS,9R)-11-(cyclopropylmethyl)-4,8a-dihydroxy-6-oxo-6,7,8,8a,9,10-hexahydro-5H-9,4b-(epiminoethano)phenanthrene-3-carboxamide

InChi Key: RYIDHLJADOKWFM-MAODMQOUSA-N

InChi Code: InChI=1S/C21H26N2O4/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26)/t16-,20-,21-/m1/s1

SMILES Code: O=C(C(C(O)=C1[C@@]23C4)=CC=C1C[C@@H](N(CC5CC5)CC3)[C@]2(O)CCC4=O)N

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

Shelf Life: >3 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: 2934.99.03.00

Preparing Stock Solutions

The following data is based on the product molecular weight 370.44 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

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1: Shram MJ, Silverman B, Ehrich E, Sellers EM, Turncliff R. Use of Remifentanil in a Novel Clinical Paradigm to Characterize Onset and Duration of Opioid Blockade by Samidorphan, a Potent μ-Receptor Antagonist. J Clin Psychopharmacol. 2015 Jun;35(3):242-9. doi: 10.1097/JCP.0000000000000320. PubMed PMID: 25928699; PubMed Central PMCID: PMC4415969.

2: Turncliff R, DiPetrillo L, Silverman B, Ehrich E. Single- and multiple-dose pharmacokinetics of samidorphan, a novel opioid antagonist, in healthy volunteers. Clin Ther. 2015 Feb 1;37(2):338-48. doi: 10.1016/j.clinthera.2014.10.001. Epub 2014 Oct 29. PubMed PMID: 25456560.

3: Ehrich E, Turncliff R, Du Y, Leigh-Pemberton R, Fernandez E, Jones R, Fava M. Evaluation of opioid modulation in major depressive disorder. Neuropsychopharmacology. 2015 May;40(6):1448-55. doi: 10.1038/npp.2014.330. Epub 2014 Dec 18. PubMed PMID: 25518754; PubMed Central PMCID: PMC4397403.

4: Fava M, Memisoglu A, Thase ME, Bodkin JA, Trivedi MH, de Somer M, Du Y, Leigh-Pemberton R, DiPetrillo L, Silverman B, Ehrich E. Opioid Modulation With Buprenorphine/Samidorphan as Adjunctive Treatment for Inadequate Response to Antidepressants: A Randomized Double-Blind Placebo-Controlled Trial. Am J Psychiatry. 2016 May 1;173(5):499-508. doi: 10.1176/appi.ajp.2015.15070921. Epub 2016 Feb 12. PubMed PMID: 26869247.

5: O'Malley SS, Todtenkopf MS, Du Y, Ehrich E, Silverman BL. Effects of the Opioid System Modulator, Samidorphan, on Measures of Alcohol Consumption and Patient Reported Outcomes in Adults with Alcohol Dependence. Alcohol Clin Exp Res. 2018 Jul 28. doi: 10.1111/acer.13849. [Epub ahead of print] PubMed PMID: 30055046.

6: Ragguett RM, Rong C, Rosenblat JD, Ho RC, McIntyre RS. Pharmacodynamic and pharmacokinetic evaluation of buprenorphine + samidorphan for the treatment of major depressive disorder. Expert Opin Drug Metab Toxicol. 2018 Apr;14(4):475-482. doi: 10.1080/17425255.2018.1459564. Epub 2018 Apr 6. Review. PubMed PMID: 29621905.

7: Silverman BL, Martin W, Memisoglu A, DiPetrillo L, Correll CU, Kane JM. A randomized, double-blind, placebo-controlled proof of concept study to evaluate samidorphan in the prevention of olanzapine-induced weight gain in healthy volunteers. Schizophr Res. 2018 May;195:245-251. doi: 10.1016/j.schres.2017.10.014. Epub 2017 Nov 20. PubMed PMID: 29158012.

8: Sun L, McDonnell D, Liu J, von Moltke L. Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine-Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study. Clin Pharmacol Drug Dev. 2018 Jul 30. doi: 10.1002/cpdd.601. [Epub ahead of print] PubMed PMID: 30059196.