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Cat. No.: HY-187603

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CGP 40215

CGP 40215 is an S-adenosylmethionine decarboxylase inhibitor with an IC₅₀ of 20.3 μM against Trypanosoma brucei brucei AdoMet decarboxylase. CGP 40215 blocks spermidine production and leads to putrescine accumulation. CGP 40215 inhibits polyamine biosynthesis in intact trypanosomes, acts synergistically with the ornithine decarboxylase inhibitor DFMO (HY-B0744) against CNS model infections, and ameliorates laboratory infections caused by multiple Trypanosoma brucei subspecies and Trypanosoma congolense isolates, including strains tolerant to standard trypanocides. CGP 40215 can be used for research on African trypanosomiasis and Chagas disease.

For research use only. We do not sell to patients.

CAS No.: 211816-91-0
Formula: C₁₇H₁₉N₉
Molecular Weight:349.39

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CGP 40215 Chemical Structure

CAS No.: 211816-91-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All Parasite Isoforms :

In Vitro

CGP 40215A (20.3 μM) inhibits Trypanosoma brucei brucei Lab 110 EATRO AdoMet decarboxylase with an IC₅₀ of 20.3 μM^[1].
Preincubation of T. brucei brucei Lab 110 EATRO with CGP 40215A (10 μM; 1 h) inhibits polyamine biosynthesis, reducing spermidine levels by 36%, increasing putrescine levels by 20%, and reducing AdoMet decarboxylase activity by 68%^[1].
CGP 40215 (0-10 mM) noncompetitively inhibits wild-type and mutant T. cruzi AdoMetDC with IC₅₀ values that are decreased by the addition of putrescine for wild-type, F285H, A5H, F7A, V52I, V64A, L221T, T245A, E247A, and C250F, while mutants S111R, D174V, and D174V/E247A lose sensitivity to putrescine-mediated changes in CGP 40215 binding^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CGP 40215A (1-25 mg/kg/day; i.p. or s.c.; 3-5 days) is curative against acute T. brucei brucei infections at 10 mg/kg/day for 3 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Swiss Webster (female, 20-25 g); Swiss ICR (female, 25-30 g)^[1]
Dosage:

1 mg/kg/day; 2.5 mg/kg/day; 5 mg/kg/day; 10 mg/kg/day; 20 mg/kg/day; 25 mg/kg/day
Administration:

i.p.; s.c.; once, twice, or three times daily; 3, 4, or 5 days
Result:

Achieved 0/15 cures at 1 mg/kg/day for 3 days (mean survival 6.5 days).
Achieved 5/10 cures at 2.5 mg/kg/day for 3 days (mean survival 12.2 days).
Achieved 13/15 cures at 5 mg/kg/day for 3 days (mean survival 19.5 days).
Achieved 10/10 cures at 10 mg/kg/day for 3 days.
Achieved 0/10 cures at 1 mg/kg/day for 5 days (mean survival 10.1 days).
Achieved 4/5 cures at 2.5 mg/kg/day for 5 days (mean survival 32 days).
Achieved 9/10 cures at 5 mg/kg/day for 5 days (mean survival 32 days).
Achieved 5/5 cures at 10 mg/kg/day for 5 days.
Achieved 5/5 cures at 10 mg/kg/day s.c. for 4 days (S427 isolate).
Achieved 4/4 cures at 5 mg/kg/day for 4 days (STIB 950 isolate).
Achieved 4/4 cures at 10 mg/kg/day for 2 days (STIB 950 isolate).
Achieved 3/4 cures at 20 mg/kg/day single dose (STIB 950 isolate, mean survival 21 days).
Achieved 5/5 cures at 5, 10, or 25 mg/kg/day for 3 days starting at 24 h postinfection.
Achieved 7/15 cures at 5 mg/kg/day for 3 days starting at 48 h postinfection (mean survival 6.1 days).
Achieved 8/15 cures at 10 mg/kg/day for 3 days starting at 48 h postinfection (mean survival 4 days).
Achieved 15/15 cures at 25 mg/kg/day for 3 days starting at 48 h postinfection.
Achieved 0/5 cures at 5 mg/kg/day for 3 days starting at 72 h postinfection (mean survival 3.4 days).
Achieved 1/5 cures at 10 mg/kg/day for 3 days starting at 72 h postinfection (mean survival 4 days).
Achieved 2/5 cures at 25 mg/kg/day for 3 days starting at 72 h postinfection (mean survival 4 days).

Chemical Information

CAS No. 211816-91-0
Molecular Weight 349.39
Formula C₁₇H₁₉N₉
SMILES

N=C(C1=CC(/C=N/NC(N/N=C/C2=CC=CC(C(N)=N)=C2)=N)=CC=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bacchi CJ, et al. In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors. Antimicrobial agents and chemotherapy. 1996 Jun;40(6):1448-53.

[2]. Volkov OA, et al. Relief of autoinhibition by conformational switch explains enzyme activation by a catalytically dead paralog. eLife. 2016 Dec 15;5:e20198.

[3]. Beswick TC, et al. Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase. Biochemistry. 2006 Jun 27;45(25):7797-807.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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