TGN-020
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MedKoo CAT#: 562281

CAS#: 51987-99-6 (free base)

Description: TGN-020 is an aquaporin 4 (AQP4) channel blocker. It acts by increasing regional cerebral blood flow and reducing ischemia-induced brain edema.


Chemical Structure

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TGN-020
CAS# 51987-99-6 (free base)

Theoretical Analysis

MedKoo Cat#: 562281
Name: TGN-020
CAS#: 51987-99-6 (free base)
Chemical Formula: C8H6N4OS
Exact Mass: 206.03
Molecular Weight: 206.220
Elemental Analysis: C, 46.59; H, 2.93; N, 27.17; O, 7.76; S, 15.55

Price and Availability

Size Price Availability Quantity
50mg USD 250 2 Weeks
100mg USD 400 2 Weeks
200mg USD 650 2 Weeks
500mg USD 1250 2 Weeks
1g USD 1850 2 Weeks
2g USD 2850 2 Weeks
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Related CAS #: 1313731-99-5 (sodium)   51987-99-6 (free base)  

Synonym: TGN-020; TGN 020; TGN020;

IUPAC/Chemical Name: N-1,3,4-Thiadiazol-2-yl-3-pyridinecarboxamide

InChi Key: AGEGZHOPKZFKBP-UHFFFAOYSA-N

InChi Code: InChI=1S/C8H6N4OS/c13-7(6-2-1-3-9-4-6)11-8-12-10-5-14-8/h1-5H,(H,11,12,13)

SMILES Code: O=C(C1=CC=CN=C1)NC2=NN=CS2

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: >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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 206.22 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: Yan X, Liu J, Wang X, Li W, Chen J, Sun H. Pretreatment with AQP4 and NKCC1 Inhibitors Concurrently Attenuated Spinal Cord Edema and Tissue Damage after Spinal Cord Injury in Rats. Front Physiol. 2018 Jan 19;9:6. doi: 10.3389/fphys.2018.00006. eCollection 2018. PubMed PMID: 29403391; PubMed Central PMCID: PMC5780344.

2: Pirici I, Balsanu TA, Bogdan C, Margaritescu C, Divan T, Vitalie V, Mogoanta L, Pirici D, Carare RO, Muresanu DF. Inhibition of Aquaporin-4 Improves the Outcome of Ischaemic Stroke and Modulates Brain Paravascular Drainage Pathways. Int J Mol Sci. 2017 Dec 23;19(1). pii: E46. doi: 10.3390/ijms19010046. PubMed PMID: 29295526; PubMed Central PMCID: PMC5795996.

3: Suzuki Y, Nakamura Y, Yamada K, Kurabe S, Okamoto K, Aoki H, Kitaura H, Kakita A, Fujii Y, Huber VJ, Igarashi H, Kwee IL, Nakada T. Aquaporin Positron Emission Tomography Differentiates Between Grade III and IV Human Astrocytoma. Neurosurgery. 2017 Jun 21. doi: 10.1093/neuros/nyx314. [Epub ahead of print] PubMed PMID: 28645205.

4: Wei F, Zhang C, Xue R, Shan L, Gong S, Wang G, Tao J, Xu G, Zhang G, Wang L. The pathway of subarachnoid CSF moving into the spinal parenchyma and the role of astrocytic aquaporin-4 in this process. Life Sci. 2017 Aug 1;182:29-40. doi: 10.1016/j.lfs.2017.05.028. Epub 2017 May 30. PubMed PMID: 28576642.

5: Popescu ES, Pirici I, Ciurea RN, Bălşeanu TA, Cătălin B, Mărgăritescu C, Mogoantă L, Hostiuc S, Pirici D. Three-dimensional organ scanning reveals brain edema reduction in a rat model of stroke treated with an aquaporin 4 inhibitor. Rom J Morphol Embryol. 2017;58(1):59-66. PubMed PMID: 28523299.

6: Kida T, Oku H, Horie T, Fukumoto M, Okuda Y, Morishita S, Ikeda T. Implication of VEGF and aquaporin 4 mediating Müller cell swelling to diabetic retinal edema. Graefes Arch Clin Exp Ophthalmol. 2017 Jun;255(6):1149-1157. doi: 10.1007/s00417-017-3631-z. Epub 2017 Mar 16. PubMed PMID: 28303331.

7: Leitão RA, Sereno J, Castelhano JM, Gonçalves SI, Coelho-Santos V, Fontes-Ribeiro C, Castelo-Branco M, Silva AP. Aquaporin-4 as a New Target against Methamphetamine-Induced Brain Alterations: Focus on the Neurogliovascular Unit and Motivational Behavior. Mol Neurobiol. 2018 Mar;55(3):2056-2069. doi: 10.1007/s12035-017-0439-0. Epub 2017 Mar 10. PubMed PMID: 28283882.

8: Nishikawa Y, Oku H, Morishita S, Horie T, Kida T, Mimura M, Fukumoto M, Kojima S, Ikeda T. Negative impact of AQP-4 channel inhibition on survival of retinal ganglion cells and glutamate metabolism after crushing optic nerve. Exp Eye Res. 2016 May;146:118-27. doi: 10.1016/j.exer.2015.12.012. Epub 2016 Jan 7. PubMed PMID: 26772436.

9: Burnett ME, Johnston HM, Green KN. Structural characterization of the aquaporin inhibitor 2-nicotinamido-1,3,4-thiadiazole. Acta Crystallogr C Struct Chem. 2015 Dec 1;71(Pt 12):1074-9. doi: 10.1107/S2053229615021130. Epub 2015 Nov 17. PubMed PMID: 26632834.

10: Igarashi H, Tsujita M, Suzuki Y, Kwee IL, Nakada T. Inhibition of aquaporin-4 significantly increases regional cerebral blood flow. Neuroreport. 2013 Apr 17;24(6):324-8. doi: 10.1097/WNR.0b013e32835fc827. PubMed PMID: 23462267.

11: Suzuki Y, Nakamura Y, Yamada K, Huber VJ, Tsujita M, Nakada T. Aquaporin-4 positron emission tomography imaging of the human brain: first report. J Neuroimaging. 2013 Apr;23(2):219-23. doi: 10.1111/j.1552-6569.2012.00704.x. Epub 2012 Jul 20. PubMed PMID: 22817997.

12: Huber VJ, Tsujita M, Nakada T. Aquaporins in drug discovery and pharmacotherapy. Mol Aspects Med. 2012 Oct-Dec;33(5-6):691-703. doi: 10.1016/j.mam.2012.01.002. Epub 2012 Jan 24. Review. PubMed PMID: 22293138.

13: Nakamura Y, Suzuki Y, Tsujita M, Huber VJ, Yamada K, Nakada T. Development of a Novel Ligand, [C]TGN-020, for Aquaporin 4 Positron Emission Tomography Imaging. ACS Chem Neurosci. 2011 Oct 19;2(10):568-571. Epub 2011 Jun 27. PubMed PMID: 22022637; PubMed Central PMCID: PMC3198134.

14: Igarashi H, Huber VJ, Tsujita M, Nakada T. Pretreatment with a novel aquaporin 4 inhibitor, TGN-020, significantly reduces ischemic cerebral edema. Neurol Sci. 2011 Feb;32(1):113-6. doi: 10.1007/s10072-010-0431-1. Epub 2010 Oct 6. PubMed PMID: 20924629; PubMed Central PMCID: PMC3026762.