CGP 40215

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

MedKoo CAT#: 412658

CAS#: 211816-91-0

Description: CGP 40215 is a specific S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor that was found to inhibit the growth of Leishmania donovani promastigotes

Chemical Structure

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CGP 40215
CAS# 211816-91-0
Instruction

Theoretical Analysis

MedKoo Cat#: 412658
Name: CGP 40215
CAS#: 211816-91-0
Chemical Formula: C17H19N9
Exact Mass: 349.18
Molecular Weight: 349.400
Elemental Analysis: C, 58.44; H, 5.48; N, 36.08

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: CGP 40215; CGP-40215; CGP40215

IUPAC/Chemical Name: 3-((E)-(((E)-amino(2-((E)-3-carbamimidoylbenzylidene)hydrazinyl)methylene)hydrazono)methyl)benzimidamide

InChi Key: NSHBIZYDZBQOQB-WDBPGAOMSA-N

InChi Code: InChI=1S/C17H19N9/c18-15(19)13-5-1-3-11(7-13)9-23-25-17(22)26-24-10-12-4-2-6-14(8-12)16(20)21/h1-10H,(H3,18,19)(H3,20,21)(H3,22,25,26)/b23-9+,24-10+

SMILES Code: N/C(N/N=C/c1cc(C(N)=N)ccc1)=N\N=C\c2cc(C(N)=N)ccc2

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: >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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 349.40 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: Beswick TC, Willert EK, Phillips MA. Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase. Biochemistry. 2006 Jun 27;45(25):7797-807. doi: 10.1021/bi0603975. PMID: 16784231.

2: Goldberg B, Rattendi D, Lloyd D, Sufrin JR, Bacchi CJ. Effects of intermediates of methionine metabolism and nucleoside analogs on S-adenosylmethionine transport by Trypanosoma brucei brucei and a drug-resistant Trypanosoma brucei rhodesiense. Biochem Pharmacol. 1998 Jul 1;56(1):95-103. doi: 10.1016/s0006-2952(98)00118-x. PMID: 9698093.

3: Mukhopadhyay R, Kapoor P, Madhubala R. Antileishmanial effect of a potent S-adenosylmethionine decarboxylase inhibitor: CGP 40215A. Pharmacol Res. 1996 Jan;33(1):67-70. doi: 10.1006/phrs.1996.0011. PMID: 8817649.

4: Heby O, Persson L, Rentala M. Targeting the polyamine biosynthetic enzymes: a promising approach to therapy of African sleeping sickness, Chagas' disease, and leishmaniasis. Amino Acids. 2007 Aug;33(2):359-66. doi: 10.1007/s00726-007-0537-9. Epub 2007 Jul 4. PMID: 17610127.

5: Das Gupta R, Krause-Ihle T, Bergmann B, Müller IB, Khomutov AR, Müller S, Walter RD, Lüersen K. 3-Aminooxy-1-aminopropane and derivatives have an antiproliferative effect on cultured Plasmodium falciparum by decreasing intracellular polyamine concentrations. Antimicrob Agents Chemother. 2005 Jul;49(7):2857-64. doi: 10.1128/AAC.49.7.2857-2864.2005. PMID: 15980361; PMCID: PMC1168667.

6: Bacchi CJ, Brun R, Croft SL, Alicea K, Bühler Y. In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors. Antimicrob Agents Chemother. 1996 Jun;40(6):1448-53. doi: 10.1128/AAC.40.6.1448. PMID: 8726018; PMCID: PMC163348.

7: Brun R, Burri C, Gichuki CW. The story of CGP 40 215: studies on its efficacy and pharmacokinetics in African green monkey infected with Trypanosoma brucei rhodesiense. Trop Med Int Health. 2001 May;6(5):362-8. doi: 10.1046/j.1365-3156.2001.00728.x. PMID: 11348531.

8: Ogbunude PO, Asiri SA. In vitro effect of diamidines on intracellular polyamines of Acanthamoeba polyphaga. Drugs Exp Clin Res. 2001;27(4):127-33. PMID: 11822222.

9: Nguyen B, Hamelberg D, Bailly C, Colson P, Stanek J, Brun R, Neidle S, Wilson WD. Characterization of a novel DNA minor-groove complex. Biophys J. 2004 Feb;86(2):1028-41. doi: 10.1016/s0006-3495(04)74178-8. PMID: 14747338; PMCID: PMC1303896.

10: Nguyen B, Lee MP, Hamelberg D, Joubert A, Bailly C, Brun R, Neidle S, Wilson WD. Strong binding in the DNA minor groove by an aromatic diamidine with a shape that does not match the curvature of the groove. J Am Chem Soc. 2002 Nov 20;124(46):13680-1. doi: 10.1021/ja027953c. PMID: 12431090.