Ganaplacide

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MedKoo CAT#: 526916

CAS#: 1261113-96-5

Description: 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

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Ganaplacide
CAS# 1261113-96-5
Instruction

Theoretical Analysis

MedKoo Cat#: 526916
Name: Ganaplacide
CAS#: 1261113-96-5
Chemical Formula: C22H23F2N5O
Exact Mass: 411.19
Molecular Weight: 411.457
Elemental Analysis: C, 64.22; H, 5.63; F, 9.23; N, 17.02; O, 3.89

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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:

Biological target:
In vitro activity:
In vivo activity:

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.

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: 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.