Ganaplacide | KAF-156 | GNF-156 | CAS#1261113-96-5

MedKoo Cat#: 526916 | Name: Ganaplacide

Description:

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

Ganaplacide, also known as KAF-156. and GNF-156 and ganaplacide, is an antimalarials potentially for treatment of Malaria. KAF156 belongs to a new class of antimalarial agents (imidazolopiperazines), with activity against asexual and sexual blood stages and the preerythrocytic liver stages of malarial parasites. KAF156 showed antimalarial activity without evident safety concerns in a small number of adults with uncomplicated P. vivax or P. falciparum malaria.

Chemical Structure

Ganaplacide

CAS#1261113-96-5

Theoretical Analysis

MedKoo Cat#: 526916

Name: Ganaplacide

CAS#: 1261113-96-5

Chemical Formula: C22H23F2N5O

Exact Mass: 411.1871

Molecular Weight: 411.46

Elemental Analysis: C, 64.22; H, 5.63; F, 9.23; N, 17.02; O, 3.89

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

KAF-156; KAF 156; KAF156; GNF-156; GNF156; GNF 156; ganaplacide;

IUPAC/Chemical Name

2-Amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-5,6-dihydro-8,8-dimethylimidazo(1,2-a)pyrazin-7(8H)-yl)ethanone

InChi Key

BUPRVECGWBHCQV-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H23F2N5O/c1-22(2)21-27-19(14-3-5-15(23)6-4-14)20(26-17-9-7-16(24)8-10-17)28(21)11-12-29(22)18(30)13-25/h3-10,26H,11-13,25H2,1-2H3

SMILES Code

CC1(C)C2=NC(C3=CC=C(F)C=C3)=C(NC4=CC=C(F)C=C4)N2CCN1C(CN)=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

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

Preparing Stock Solutions

The following data is based on the product molecular weight 411.46 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

1: White NJ, Duong TT, Uthaisin C, Nosten F, Phyo AP, Hanboonkunupakarn B, Pukrittayakamee S, Jittamala P, Chuthasmit K, Cheung MS, Feng Y, Li R, Magnusson B, Sultan M, Wieser D, Xun X, Zhao R, Diagana TT, Pertel P, Leong FJ. Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria. N Engl J Med. 2016 Sep 22;375(12):1152-60. doi: 10.1056/NEJMoa1602250. PubMed PMID: 27653565. 2: Lim MY, LaMonte G, Lee MC, Reimer C, Tan BH, Corey V, Tjahjadi BF, Chua A, Nachon M, Wintjens R, Gedeck P, Malleret B, Renia L, Bonamy GM, Ho PC, Yeung BK, Chow ED, Lim L, Fidock DA, Diagana TT, Winzeler EA, Bifani P. UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes. Nat Microbiol. 2016 Sep 19;1:16166. doi: 10.1038/nmicrobiol.2016.166. PubMed PMID: 27642791. 3: Huskey SE, Forseth RR, Li H, Jian Z, Catoire A, Zhang J, Ray T, He H, Flarakos J, Mangold JB. Utilization of Stable Isotope Labeling to Facilitate the Identification of Polar Metabolites of KAF156, an Antimalarial Agent. Drug Metab Dispos. 2016 Oct;44(10):1697-708. doi: 10.1124/dmd.116.072108. Epub 2016 Aug 2. PubMed PMID: 27486238. 4: Mischlinger J, Agnandji ST, Ramharter M. Single dose treatment of malaria - current status and perspectives. Expert Rev Anti Infect Ther. 2016 Jul;14(7):669-78. doi: 10.1080/14787210.2016.1192462. Epub 2016 Jun 7. PubMed PMID: 27254098. 5: Diagana TT. Supporting malaria elimination with 21st century antimalarial agent drug discovery. Drug Discov Today. 2015 Oct;20(10):1265-70. doi: 10.1016/j.drudis.2015.06.009. Epub 2015 Jun 21. Review. PubMed PMID: 26103616. 6: Held J, Jeyaraj S, Kreidenweiss A. Antimalarial compounds in Phase II clinical development. Expert Opin Investig Drugs. 2015 Mar;24(3):363-82. doi: 10.1517/13543784.2015.1000483. Epub 2015 Jan 7. Review. PubMed PMID: 25563531. 7: Leong FJ, Zhao R, Zeng S, Magnusson B, Diagana TT, Pertel P. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014 Nov;58(11):6437-43. doi: 10.1128/AAC.03478-14. Epub 2014 Aug 18. PubMed PMID: 25136017; PubMed Central PMCID: PMC4249437. 8: Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A, Barnes SW, Plouffe D, Lee MC, Fidock DA, Graumans W, van de Vegte-Bolmer M, van Gemert GJ, Wirjanata G, Sebayang B, Marfurt J, Russell B, Suwanarusk R, Price RN, Nosten F, Tungtaeng A, Gettayacamin M, Sattabongkot J, Taylor J, Walker JR, Tully D, Patra KP, Flannery EL, Vinetz JM, Renia L, Sauerwein RW, Winzeler EA, Glynne RJ, Diagana TT. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7. doi: 10.1128/AAC.02727-13. Epub 2014 Jun 9. PubMed PMID: 24913172; PubMed Central PMCID: PMC4135840.