MedKoo Biosciences

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

MedKoo CAT#: 319738

CAS#: 870070-55-6

Description: Tozadenant, also known as RO-4494351 and SYN115, is an oral, selective adenosine A2A receptor antagonist that improves motor function in animal models of Parkinson's disease. Adenosine A(2a) receptor antagonists reduce symptom severity in Parkinson disease (PD) and animal models. Rodent studies support the hypothesis that A(2a) antagonists produce this benefit by reducing the inhibitory output of the basal ganglia indirect pathway.

Chemical Structure

Tozadenant

CAS# 870070-55-6

Instruction

Theoretical Analysis

MedKoo Cat#: 319738
Name: Tozadenant
CAS#: 870070-55-6
Chemical Formula: C19H26N4O4S
Exact Mass: 406.17
Molecular Weight: 406.501
Elemental Analysis: C, 56.14; H, 6.45; N, 13.78; O, 15.74; S, 7.89

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
25mg	USD 270
50mg	USD 450
100mg	USD 720
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: RO-4494351; RO4494351; RO 4494351; SYN115; SYN-115; SYN 115; RO4494351-002; RO4494351-000; Tozadenant

IUPAC/Chemical Name: 4-hydroxy-N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide

InChi Key: XNBRWUQWSKXMPW-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H26N4O4S/c1-19(25)5-7-23(8-6-19)18(24)21-17-20-15-14(26-2)4-3-13(16(15)28-17)22-9-11-27-12-10-22/h3-4,25H,5-12H2,1-2H3,(H,20,21,24)

SMILES Code: O=C(N1CCC(C)(O)CC1)NC2=NC3=C(OC)C=CC(N4CCOCC4)=C3S2

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

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 406.50 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:

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1: Michel A, Downey P, Van Damme X, De Wolf C, Schwarting R, Scheller D. Behavioural Assessment of the A2a/NR2B Combination in the Unilateral 6-OHDA-Lesioned Rat Model: A New Method to Examine the Therapeutic Potential of Non-Dopaminergic Drugs. PLoS One. 2015 Aug 31;10(8):e0135949. doi: 10.1371/journal.pone.0135949. eCollection 2015. PubMed PMID: 26322641; PubMed Central PMCID: PMC4555651.

2: Rascol O, Perez-Lloret S, Ferreira JJ. New treatments for levodopa-induced motor complications. Mov Disord. 2015 Sep 15;30(11):1451-60. doi: 10.1002/mds.26362. Epub 2015 Aug 21. Review. PubMed PMID: 26293004.

3: Stewart SB, Koller JM, Campbell MC, Black KJ. Arterial spin labeling versus BOLD in direct challenge and drug-task interaction pharmacological fMRI. PeerJ. 2014 Dec 11;2:e687. doi: 10.7717/peerj.687. eCollection 2014. PubMed PMID: 25538867; PubMed Central PMCID: PMC4266850.

4: Michel A, Downey P, Nicolas JM, Scheller D. Unprecedented therapeutic potential with a combination of A2A/NR2B receptor antagonists as observed in the 6-OHDA lesioned rat model of Parkinson's disease. PLoS One. 2014 Dec 16;9(12):e114086. doi: 10.1371/journal.pone.0114086. eCollection 2014. PubMed PMID: 25513815; PubMed Central PMCID: PMC4267740.

5: Barret O, Hannestad J, Alagille D, Vala C, Tavares A, Papin C, Morley T, Fowles K, Lee H, Seibyl J, Tytgat D, Laruelle M, Tamagnan G. Adenosine 2A receptor occupancy by tozadenant and preladenant in rhesus monkeys. J Nucl Med. 2014 Oct;55(10):1712-8. doi: 10.2967/jnumed.114.142067. Epub 2014 Jul 31. PubMed PMID: 25082853.

6: Hauser RA, Olanow CW, Kieburtz KD, Pourcher E, Docu-Axelerad A, Lew M, Kozyolkin O, Neale A, Resburg C, Meya U, Kenney C, Bandak S. Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76. doi: 10.1016/S1474-4422(14)70148-6. Epub 2014 Jul 6. PubMed PMID: 25008546.

7: Pinna A. Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued. CNS Drugs. 2014 May;28(5):455-74. doi: 10.1007/s40263-014-0161-7. Review. PubMed PMID: 24687255.

8: Perez-Lloret S, Merello M. Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant. Expert Opin Pharmacother. 2014 Jun;15(8):1097-107. doi: 10.1517/14656566.2014.903924. Epub 2014 Mar 27. Review. PubMed PMID: 24673462.

9: Pytka K, Zygmunt M, Filipek B. [Pharmacotherapy of Parkinson's disease: progress or regress?]. Postepy Hig Med Dosw (Online). 2013 Jul 24;67:700-8. Review. Polish. PubMed PMID: 24018435.

10: Lane S, Green C, Steinberg J, Ma L, Schmitz J, Rathnayaka N, Bandak S, Ferre S, Moeller F. Cardiovascular and Subjective Effects of the Novel Adenosine A(2A) Receptor Antagonist SYN115 in Cocaine Dependent Individuals. J Addict Res Ther. 2012 Mar 28;S1. pii: 009. PubMed PMID: 22905331; PubMed Central PMCID: PMC3419540.

11: Moeller FG, Steinberg JL, Lane SD, Kjome KL, Ma L, Ferre S, Schmitz JM, Green CE, Bandak SI, Renshaw PF, Kramer LA, Narayana PA. Increased Orbitofrontal Brain Activation after Administration of a Selective Adenosine A(2A) Antagonist in Cocaine Dependent Subjects. Front Psychiatry. 2012 May 28;3:44. doi: 10.3389/fpsyt.2012.00044. eCollection 2012. PubMed PMID: 22654774; PubMed Central PMCID: PMC3361057.

12: Hauser RA. Future treatments for Parkinson's disease: surfing the PD pipeline. Int J Neurosci. 2011;121 Suppl 2:53-62. doi: 10.3109/00207454.2011.620195. Review. PubMed PMID: 22035030.

13: Black KJ, Koller JM, Campbell MC, Gusnard DA, Bandak SI. Quantification of indirect pathway inhibition by the adenosine A2a antagonist SYN115 in Parkinson disease. J Neurosci. 2010 Dec 1;30(48):16284-92. doi: 10.1523/JNEUROSCI.2590-10.2010. PubMed PMID: 21123574; PubMed Central PMCID: PMC3008651.

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