SAGE-217
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MedKoo CAT#: 555380

CAS#: 1632051-40-1 (free base)

Description: SAGE-217 is a potent GABAA receptor agonist ( EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors). SAGE-217 is a potent GABAA receptor modulator at both synaptic and extrasynaptic receptor subtypes, with excellent oral DMPK properties. SAGE-217 has completed a phase 1 single ascending dose (SAD) and multiple ascending dose (MAD) clinical trial and is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD), major depressive disorder (MDD), and essential tremor (ET).


Price and Availability

Size
Price

100mg
USD 1650
1g
USD 4950
Size
Price

200mg
USD 2450
2g
USD 8950
Size
Price

500mg
USD 3650

SAGE-217, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555380
Name: SAGE-217
CAS#: 1632051-40-1 (free base)
Chemical Formula: C25H35N3O2
Exact Mass: 409.2729
Molecular Weight: 409.574
Elemental Analysis: C, 73.31; H, 8.61; N, 10.26; O, 7.81


Synonym: SAGE-217; SAGE 217; SAGE217;

IUPAC/Chemical Name: 1-[2-[(3R,5R,8R,9R,10S,13S,14S,17S)-3-hydroxy-3,13-dimethyl-2,4,5,6,7,8,9,10,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl]pyrazole-4-carbonitrile

InChi Key: HARRKNSQXBRBGZ-GVKWWOCJSA-N

InChi Code: InChI=1S/C25H35N3O2/c1-24(30)9-7-18-17(11-24)3-4-20-19(18)8-10-25(2)21(20)5-6-22(25)23(29)15-28-14-16(12-26)13-27-28/h13-14,17-22,30H,3-11,15H2,1-2H3/t17-,18+,19-,20-,21+,22-,24-,25+/m1/s1

SMILES Code: O=C([C@H]1CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@](C)(O)CC[C@]4([H])[C@@]3([H])CC[C@]12C)CN5C=C(C=N5)C#N


Technical Data

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).

Harmonized System Code:
2934.99.03.00


References

1: Wilkinson ST, Sanacora G. A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. Drug Discov Today. 2018 Nov 14. pii: S1359-6446(18)30376-3. doi: 10.1016/j.drudis.2018.11.007. [Epub ahead of print] Review. PubMed PMID: 30447328.

2: Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Blanco MJ, Belfort GM, Dai J, Loya CM, Ackley MA, Althaus AL, Grossman SJ, Hoffmann E, Doherty JJ, Robichaud AJ. Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)(A) Receptor. J Med Chem. 2017 Sep 28;60(18):7810-7819. doi: 10.1021/acs.jmedchem.7b00846. Epub 2017 Aug 17. PubMed PMID: 28753313.

3: Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS. Progress report on new antiepileptic drugs: A summary of the Thirteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XIII). Epilepsia. 2017 Feb;58(2):181-221. doi: 10.1111/epi.13634. Epub 2017 Jan 23. Review. PubMed PMID: 28111749.

4: Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS. Progress report on new antiepileptic drugs: A summary of the Twelfth Eilat Conference (EILAT XII). Epilepsy Res. 2015 Mar;111:85-141. doi: 10.1016/j.eplepsyres.2015.01.001. Epub 2015 Jan 19. Review. PubMed PMID: 25769377.