WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H326679
CAS#: 117928-94-6 (free base)
Description: Rapastinel, also known as GLYX 13 and BV 102, is a monoclonal antibody-derived tetrapeptide that acts as a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor.
Hodoodo Cat#: H326679
Name: Rapastinel
CAS#: 117928-94-6 (free base)
Chemical Formula: C18H31N5O6
Exact Mass: 413.23
Molecular Weight: 413.480
Elemental Analysis: C, 52.29; H, 7.56; N, 16.94; O, 23.22
Related CAS #: 491872-39-0 (acetate) 117928-94-6 (free base)
Synonym: GLYX-13; GLYX 13; GLYX13; BV-102; BV102; BV 102; TPPT-amide; Rapastinel
IUPAC/Chemical Name: (S)-1-(L-threonyl-L-prolyl)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)pyrrolidine-2-carboxamide
InChi Key: GIBQQARAXHVEGD-BSOLPCOYSA-N
InChi Code: InChI=1S/C18H31N5O6/c1-9(24)13(19)18(29)23-8-4-6-12(23)17(28)22-7-3-5-11(22)16(27)21-14(10(2)25)15(20)26/h9-14,24-25H,3-8,19H2,1-2H3,(H2,20,26)(H,21,27)/t9-,10-,11+,12+,13+,14+/m1/s1
SMILES Code: C[C@@H](O)[C@@H](C(N)=O)NC([C@H]1N(C([C@H]2N(C([C@H]([C@H](O)C)N)=O)CCC2)=O)CCC1)=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 DMSO, DMF, and ethanol
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO, DMF, and ethanol
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:
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The following data is based on the product molecular weight 413.48 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Moskal JR, Burgdorf JS, Stanton PK, Kroes RA, Disterhoft JF, Burch RM, Amin Khan M. The Development of Rapastinel (Formerly GLYX-13); a rapid acting and long lasting antidepressant. Curr Neuropharmacol. 2016 Mar 21. [Epub ahead of print] PubMed PMID: 26997507.
2: Panksepp J. Affective preclinical modeling of psychiatric disorders: taking imbalanced primal emotional feelings of animals seriously in our search for novel antidepressants. Dialogues Clin Neurosci. 2015 Dec;17(4):363-79. PubMed PMID: 26869838; PubMed Central PMCID: PMC4734875.
3: Rajagopal L, Burgdorf JS, Moskal JR, Meltzer HY. GLYX-13 (rapastinel) ameliorates subchronic phencyclidine- and ketamine-induced declarative memory deficits in mice. Behav Brain Res. 2016 Feb 15;299:105-10. doi: 10.1016/j.bbr.2015.10.060. Epub 2015 Nov 26. PubMed PMID: 26632337; PubMed Central PMCID: PMC4721234.
4: Javelot H. [Psychopharmacology of anxiety and depression: Historical aspects, current treatments and perspectives]. Ann Pharm Fr. 2016 Mar;74(2):93-118. doi: 10.1016/j.pharma.2015.09.001. Epub 2015 Oct 16. Review. French. PubMed PMID: 26472602.
5: Newport DJ, Carpenter LL, McDonald WM, Potash JB, Tohen M, Nemeroff CB; APA Council of Research Task Force on Novel Biomarkers and Treatments. Ketamine and Other NMDA Antagonists: Early Clinical Trials and Possible Mechanisms in Depression. Am J Psychiatry. 2015 Oct;172(10):950-66. doi: 10.1176/appi.ajp.2015.15040465. Review. PubMed PMID: 26423481.
6: Burgdorf J, Zhang XL, Weiss C, Gross A, Boikess SR, Kroes RA, Khan MA, Burch RM, Rex CS, Disterhoft JF, Stanton PK, Moskal JR. The long-lasting antidepressant effects of rapastinel (GLYX-13) are associated with a metaplasticity process in the medial prefrontal cortex and hippocampus. Neuroscience. 2015 Nov 12;308:202-11. doi: 10.1016/j.neuroscience.2015.09.004. Epub 2015 Sep 4. PubMed PMID: 26343295; PubMed Central PMCID: PMC4721228.
7: Burgdorf J, Kroes RA, Zhang XL, Gross AL, Schmidt M, Weiss C, Disterhoft JF, Burch RM, Stanton PK, Moskal JR. Rapastinel (GLYX-13) has therapeutic potential for the treatment of post-traumatic stress disorder: Characterization of a NMDA receptor-mediated metaplasticity process in the medial prefrontal cortex of rats. Behav Brain Res. 2015 Nov 1;294:177-85. doi: 10.1016/j.bbr.2015.07.039. Epub 2015 Jul 22. PubMed PMID: 26210936; PubMed Central PMCID: PMC4702501.