Tideglusib
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MedKoo CAT#: 522498

CAS#: 865854-05-3

Description: Tideglusib, also known as NP031112, is a GSK-3 inhibitor, which is currently under clinical trial for Alzheimer's disease. Tideglusib protects neural stem cells against NMDA receptor overactivation. Tideglusib reduces progression of brain atrophy in progressive supranuclear palsy in a randomized trial. Tideglusib prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders.


Chemical Structure

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Tideglusib
CAS# 865854-05-3

Theoretical Analysis

MedKoo Cat#: 522498
Name: Tideglusib
CAS#: 865854-05-3
Chemical Formula: C19H14N2O2S
Exact Mass: 334.0776
Molecular Weight: 334.393
Elemental Analysis: C, 68.25; H, 4.22; N, 8.38; O, 9.57; S, 9.59

Size Price Shipping out time Quantity
50mg USD 150 Same day
100mg USD 250 Same day
200mg USD 450 Same day
500mg USD 750 Same day
1g USD 1250 Same day
2g USD 2250 Same day
5g USD 4850 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-27. Prices are subject to change without notice.

Tideglusib, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: NP031112; NP 031112; NP-031112; Tideglusib.

IUPAC/Chemical Name: 2-(1-naphthalenyl)-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione

InChi Key: PMJIHLSCWIDGMD-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2

SMILES Code: O=C(N1CC2=CC=CC=C2)N(C3=C4C=CC=CC4=CC=C3)SC1=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, not in water

Shelf Life:
>2 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:
2934.99.9001

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 334.393 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.

Select a batch to recalculate based on the batch molecular weight:
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: Koros C, Stamelou M. Interventions in progressive supranuclear palsy. Parkinsonism Relat Disord. 2015 Sep 25. pii: S1353-8020(15)00424-1. doi: 10.1016/j.parkreldis.2015.09.033. [Epub ahead of print] PubMed PMID: 26459661.

2: Sun A, Li C, Chen R, Huang Y, Chen Q, Cui X, Liu H, Thrasher JB, Li B. GSK-3β controls autophagy by modulating LKB1-AMPK pathway in prostate cancer cells. Prostate. 2015 Oct 6. doi: 10.1002/pros.23106. [Epub ahead of print] PubMed PMID: 26440826.

3: Eschlböck S, Krismer F, Wenning GK. Interventional trials in atypical parkinsonism. Parkinsonism Relat Disord. 2015 Sep 25. pii: S1353-8020(15)00429-0. doi: 10.1016/j.parkreldis.2015.09.038. [Epub ahead of print] PubMed PMID: 26421389.

4: Armagan G, Keser A, Atalayın Ç, Dagcı T. Tideglusib protects neural stem cells against NMDA receptor overactivation. Pharmacol Rep. 2015 Oct;67(5):823-31. doi: 10.1016/j.pharep.2015.01.007. Epub 2015 Jan 23. PubMed PMID: 26398371.

5: Poewe W, Mahlknecht P, Krismer F. Therapeutic advances in multiple system atrophy and progressive supranuclear palsy. Mov Disord. 2015 Sep 15;30(11):1528-38. doi: 10.1002/mds.26334. Epub 2015 Jul 30. Review. PubMed PMID: 26227071.

6: Moretti DV. Are there treatments for atypical parkinsonism? An update on actual options. Rev Neurosci. 2015 Oct 1;26(5):547-53. doi: 10.1515/revneuro-2015-0008. PubMed PMID: 26098698.

7: Lovestone S, Boada M, Dubois B, Hüll M, Rinne JO, Huppertz HJ, Calero M, Andrés MV, Gómez-Carrillo B, León T, del Ser T; ARGO investigators. A phase II trial of tideglusib in Alzheimer's disease. J Alzheimers Dis. 2015;45(1):75-88. doi: 10.3233/JAD-141959. PubMed PMID: 25537011.

8: Tolosa E, Litvan I, Höglinger GU, Burn D, Lees A, Andrés MV, Gómez-Carrillo B, León T, Del Ser T; TAUROS Investigators. A phase 2 trial of the GSK-3 inhibitor tideglusib in progressive supranuclear palsy. Mov Disord. 2014 Apr;29(4):470-8. doi: 10.1002/mds.25824. Epub 2014 Feb 14. PubMed PMID: 24532007.

9: Höglinger GU, Huppertz HJ, Wagenpfeil S, Andrés MV, Belloch V, León T, Del Ser T; TAUROS MRI Investigators. Tideglusib reduces progression of brain atrophy in progressive supranuclear palsy in a randomized trial. Mov Disord. 2014 Apr;29(4):479-87. doi: 10.1002/mds.25815. Epub 2014 Jan 31. PubMed PMID: 24488721.

10: Morales-Garcia JA, Luna-Medina R, Alonso-Gil S, Sanz-Sancristobal M, Palomo V, Gil C, Santos A, Martinez A, Perez-Castillo A. Glycogen synthase kinase 3 inhibition promotes adult hippocampal neurogenesis in vitro and in vivo. ACS Chem Neurosci. 2012 Nov 21;3(11):963-71. doi: 10.1021/cn300110c. Epub 2012 Sep 24. PubMed PMID: 23173075; PubMed Central PMCID: PMC3503340.

11: del Ser T, Steinwachs KC, Gertz HJ, Andrés MV, Gómez-Carrillo B, Medina M, Vericat JA, Redondo P, Fleet D, León T. Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: a pilot study. J Alzheimers Dis. 2013;33(1):205-15. doi: 10.3233/JAD-2012-120805. PubMed PMID: 22936007.

12: Domínguez JM, Fuertes A, Orozco L, del Monte-Millán M, Delgado E, Medina M. Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904. doi: 10.1074/jbc.M111.306472. Epub 2011 Nov 18. PubMed PMID: 22102280; PubMed Central PMCID: PMC3256883.

13: Martinez A, Gil C, Perez DI. Glycogen synthase kinase 3 inhibitors in the next horizon for Alzheimer's disease treatment. Int J Alzheimers Dis. 2011;2011:280502. doi: 10.4061/2011/280502. Epub 2011 Jun 30. PubMed PMID: 21760986; PubMed Central PMCID: PMC3132520.

14: Luna-Medina R, Cortes-Canteli M, Sanchez-Galiano S, Morales-Garcia JA, Martinez A, Santos A, Perez-Castillo A. NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders. J Neurosci. 2007 May 23;27(21):5766-76. PubMed PMID: 17522320.