MedKoo Biosciences

Tafenoquine-d3 succinate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 330189

CAS#: 1133378-83-2 (d3)

Description: Tafenoquine-d3 is a trideuerium-labeled Tafenoquine derivative. Tafenoquine, also known as WR-238605, is an oral active antimalaria drug that is being investigated as a potential treatment for malaria, as well as for malaria prevention. Tafenoquine Shows Activity against Trypanosoma brucei. Tafenoquine targets leishmania respiratory complex III and induces apoptosis. Tafenoquine has a long half-life of approximately 14 days and is generally safe and well tolerated, Malaria remains an important cause of global morbidity and mortality. As antimalarial drug resistance escalates, new safe and effective medications are necessary to prevent and treat malarial infection.

Chemical Structure

Tafenoquine-d3 succinate

CAS# 1133378-83-2 (d3)

Instruction

Theoretical Analysis

MedKoo Cat#: 330189
Name: Tafenoquine-d3 succinate
CAS#: 1133378-83-2 (d3)
Chemical Formula: C28H31D3F3N3O7
Exact Mass: 466.23
Molecular Weight: 584.610
Elemental Analysis: C, 57.53; H, 6.38; F, 9.75; N, 7.19; O, 19.16

Price and Availability

Size	Price	Availability
1mg	USD 250	Ready to ship
5mg	USD 650	Ready to ship
10mg	USD 1150	Ready to ship
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.

Related CAS #: 106635-80-7 (free base), 106635-81-8 (succinate), 1133378-83-2 (d3),

Synonym: WR-238605, WR 238605, WR238605, Tafenoquine; trideuerium-labeled Tafenoquine derivative; Tafenoquine-d3 succinate

IUPAC/Chemical Name: N4-(6-methoxy-2-(methoxy-d3)-4-methyl-5-(3-(trifluoromethyl)phenoxy)quinolin-8-yl)pentane-1,4-diamine succinoic acid

InChi Key: CQBKFGJRAOXYIP-NXIGQQGZSA-N

InChi Code: InChI=1S/C24H28F3N3O3.C4H6O4/c1-14-11-20(32-4)30-22-18(29-15(2)7-6-10-28)13-19(31-3)23(21(14)22)33-17-9-5-8-16(12-17)24(25,26)27;5-3(6)1-2-4(7)8/h5,8-9,11-13,15,29H,6-7,10,28H2,1-4H3;1-2H2,(H,5,6)(H,7,8)/i4D3;

SMILES Code: CC(NC1=C2N=C(OC([2H])([2H])[2H])C=C(C)C2=C(OC3=CC=CC(C(F)(F)F)=C3)C(OC)=C1)CCCN.O=C(O)CCC(O)=O

Appearance: Light yellow 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).

HS Tariff Code: 2934.99.9001

Product Data:

Product Data

Instruction:

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Preparing Stock Solutions

The following data is based on the product molecular weight 584.610000000000000000000000000000 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

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1: Haston JC, Hwang J, Tan KR. Guidance for Using Tafenoquine for Prevention and Antirelapse Therapy for Malaria - United States, 2019. MMWR Morb Mortal Wkly Rep. 2019 Nov 22;68(46):1062-1068. doi: 10.15585/mmwr.mm6846a4. Review. PubMed PMID: 31751320. 2: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548428/ PubMed PMID: 31643747. 3: Tafenoquine succinate for malaria prevention. Aust Prescr. 2019 Jun;42(3):110-111. doi: 10.18773/austprescr.2019.034. Epub 2019 Apr 24. Review. PubMed PMID: 31363314; PubMed Central PMCID: PMC6594846. 4: Hounkpatin AB, Kreidenweiss A, Held J. Clinical utility of tafenoquine in the prevention of relapse of Plasmodium vivax malaria: a review on the mode of action and emerging trial data. Infect Drug Resist. 2019 Mar 6;12:553-570. doi: 10.2147/IDR.S151031. eCollection 2019. Review. PubMed PMID: 30881061; PubMed Central PMCID: PMC6411314. 5: Berman J, Brown T, Dow G, Toovey S. Tafenoquine and primaquine do not exhibit clinical neurologic signs associated with central nervous system lesions in the same manner as earlier 8-aminoquinolines. Malar J. 2018 Nov 6;17(1):407. doi: 10.1186/s12936-018-2555-3. Review. PubMed PMID: 30400893; PubMed Central PMCID: PMC6219089. 6: Frampton JE. Tafenoquine: First Global Approval. Drugs. 2018 Sep;78(14):1517-1523. doi: 10.1007/s40265-018-0979-2. Review. PubMed PMID: 30229442. 7: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK525504/ PubMed PMID: 30222296. 8: Dow G, Smith B. The blood schizonticidal activity of tafenoquine makes an essential contribution to its prophylactic efficacy in nonimmune subjects at the intended dose (200 mg). Malar J. 2017 May 19;16(1):209. doi: 10.1186/s12936-017-1862-4. Review. PubMed PMID: 28526056; PubMed Central PMCID: PMC5438551. 9: Ebstie YA, Abay SM, Tadesse WT, Ejigu DA. Tafenoquine and its potential in the treatment and relapse prevention of Plasmodium vivax malaria: the evidence to date. Drug Des Devel Ther. 2016 Jul 26;10:2387-99. doi: 10.2147/DDDT.S61443. eCollection 2016. Review. PubMed PMID: 27528800; PubMed Central PMCID: PMC4970641. 10: Rajapakse S, Rodrigo C, Fernando SD. Tafenoquine for preventing relapse in people with Plasmodium vivax malaria. Cochrane Database Syst Rev. 2015 Apr 29;(4):CD010458. doi: 10.1002/14651858.CD010458.pub2. Review. PubMed PMID: 25921416; PubMed Central PMCID: PMC4468925. 11: Crockett M, Kain KC. Tafenoquine: a promising new antimalarial agent. Expert Opin Investig Drugs. 2007 May;16(5):705-15. Review. PubMed PMID: 17461742. 12: Peters W. The evolution of tafenoquine--antimalarial for a new millennium? J R Soc Med. 1999 Jul;92(7):345-52. Review. PubMed PMID: 10615272; PubMed Central PMCID: PMC1297286.

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