Trypanosoma

Trypanosoma spp. are divergent protozoan parasites that cause human African trypanosomiasis, Chagas disease, and animal trypanosomiasis^[1]^[2]. Their core biology centers on stage-specific adaptation between mammalian hosts and insect vectors, requiring changes in morphology, organelle positioning, surface biology, and gene expression^[2]^[3]. Mechanistically, kinetoplastids contain glycosomes that compartmentalize major glycolytic and pentose-phosphate enzymes, supporting energy and carbohydrate metabolism^[4]. cAMP signaling differs from mammalian pathways because trypanosomatids lack G-protein-coupled receptors, possess structurally different adenylyl cyclases, and express class 1 cyclic nucleotide phosphodiesterases PDEA-D^[5]. Compared with related isoforms, only T. brucei PDEB, expressed as PDEB1 and PDEB2, has been reported essential after ablation^[5]. Disease models use T. brucei to study bloodstream infection, tsetse-vector differentiation, antigenic variation, cytokinesis, and drug discovery^[2]^[3]. For experimental intervention, N-myristoyltransferase inhibition causes trypanosomatid cell death, compromises virulence, and cures T. brucei infection in rodents^[6]. Neuropeptides also kill T. brucei by disrupting lysosome integrity, redistributing glycolytic enzymes, and inducing autophagic-like cell death^[7].

References:

[1]. Lopes AH, et al. Trypanosomatids: odd organisms, devastating diseases. Open Parasitol J. 2010;4:30-59.

[2]. Dean S. Basic Biology of Trypanosoma brucei with Reference to the Development of Chemotherapies. Curr Pharm Des. 2021;27(14):1650-1670.

[3]. Matthews KR. The developmental cell biology of Trypanosoma brucei. J Cell Sci. 2005 Jan 15;118(Pt 2):283-90. doi: 10.1242/jcs.01649. Erratum in: J Cell Sci. 2005 May 1;118(Pt 9):2078. PMID: 15654017; PMCID: PMC2686837. et al. The developmental cell biology of Trypanosoma brucei. J Cell Sci. 2005 Jan 15;118(Pt 2):283-90.

[4]. Hannaert V, et al. Evolution of energy metabolism and its compartmentation in Kinetoplastida. Kinetoplastid Biology and Disease. 2003;2:11.

[5]. Tagoe DN, et al. The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference! Front Pharmacol. 2015 Sep 7;6:185.

[6]. Goldston AM, et al. Acylation in trypanosomatids: an essential process and potential drug target. Trends Parasitol. 2014 Jul;30(7):350-60.

[7]. Delgado M, et al. Neuropeptides kill African trypanosomes by targeting intracellular compartments and inducing autophagic-like cell death. Cell Death Differ. 2009 Mar;16(3):406-16.

Trypanosoma Inhibitors (66)

Trypanosoma Related Products (73):

By Type:	Pan (7) Selective (4)

Cat. No.	Product Name	Effect	Purity

HY-B0744

Eflornithine		99.87%
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

HY-B0744B

Eflornithine hydrochloride hydrate	Inhibitor	99.90%
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

HY-12404

Diminazene aceturate	Inhibitor	99.39%
Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.

HY-B0537

Pentamidine	Inhibitor
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite *Leishmania infantum* with an IC₅₀ of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

HY-12054

Hesperadin	Inhibitor	98.89%
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

HY-183747

Antitrypanosomal agent 32	Inhibitor
Antitrypanosomal agent 32 is a antitrypanosomal agent with nanomolar potency against multiple Trypanosoma cruzi strains, including CL-Brener, Y, Dm28c-Luc and Tulahuen. Antitrypanosomal agent 32 sustains inhibition of parasite growth after washing and reduces parasitemia levels in BALB/c mice. Antitrypanosomal agent 32 can be used for the research of trypanosome infection.

HY-105111

P-536	Inhibitor
P-536 is a ACE inhibitor that also inhibits herpes simplex virus HSV-1 thymidine kinase and Trypanosoma cruzi RNA polymerase. By inhibiting the renin-angiotensin system, downregulating the expression of AT1R and NOX4, and reducing oxidative stress (decreasing plasma hydrogen peroxide (H₂O₂) and 8-isoprostaglandin levels), P-536 effectively reduces systolic blood pressure and improves vascular reactivity. P-536 also inhibits the replication of DNA/RNA viruses such as HSV-1 by blocking nucleotide metabolism and nucleic acid synthesis, competitively inhibits RNA synthesis in Trypanosoma cruzi, and inhibits amastigote replication, thereby impeding its growth. P-536 is suitable for research on hypertension, insulin resistance, and Chagas disease.

HY-112252

MDL 73811	Inhibitor
MDL 73811 is a potent AdoMetDC inhibitor and anti-trypanosomal compound. MDL 73811 has curative efficacy in a hemolymphatic model of HAT.

HY-B0537B

Pentamidine isethionate	Inhibitor	99.95%
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite *Leishmania infantum* with an IC₅₀ of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

HY-14989

SQ109	Inhibitor	99.58%
SQ109 is a potent inhibitor of the trypomastigote form of the parasite, with IC₅₀ for cell killing of 50±8 nM. SQ109, targets MmpL3, is an antitubercular agent.

HY-119293

K777	Inhibitor	99.14%
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

HY-103056

DDD85646		99.72%
DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC₅₀=2 nM; hNMT IC₅₀=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis.

HY-B0744A

Eflornithine hydrochloride		99.90%
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

HY-142021

Z-Leu-Arg-AMC		99.24%
Z-Leu-Arg-AMC is a fluorogenic peptide substrate for cysteine proteases (e.g., Cathepsin) (Ex=350 nm，Em=460 nm). Z-Leu-Arg-AMC is preferentially cleaved by Cathepsin K and S under weakly acidic conditions, while its hydrolysis relies on residual Cathepsin S activity at neutral pH. Z-Leu-Arg-AMC serves as a substrate for recombinant Sphenophorus levis Cathepsin L, falcipain-2, falcipain-3, berghepain-2, knowlepain-2, vivapain-2, as well as falcipain-2 chimeras and constructs. It enables quantitative detection of cysteine protease activity in human inflammatory bronchoalveolar lavage fluid via fluorescence generation. Z-Leu-Arg-AMC can be used in research related to pulmonary inflammatory diseases and malaria.

HY-19910

Acoziborole	Inhibitor	99.78%
Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the *T. b. brucei* S427 strain, the MIC value for SCYX-7158 is 0.6 μg/mL.

HY-N2230

N-p-trans-Coumaroyltyramine	Inhibitor	99.28%
N-p-trans-Coumaroyltyramine is a natural phenolic amide compound and an inhibitor of AChE (IC₅₀: 122 μM) and α-glucosidase (IC₅₀: 2.7 μM). N-p-trans-Coumaroyltyramine also has anti-trypanosomal activity, with an IC₅₀ of 13.3 µM against T. brucei rhodesiense. N-p-trans-Coumaroyltyramine can be used in the research of diseases such as Alzheimer's disease.

HY-B1548

Benznidazole	Inhibitor	99.90%
Benznidazole (Ro 07-1051) is an antiparasitic medication, with an IC₅₀ of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease.

HY-N7266

Obtusifoliol	Inhibitor	99.86%
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with K_d values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively.

HY-13801

Fexinidazole	Inhibitor	99.92%
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.

HY-N0397

Harpagide	Inhibitor	98.93%
Harpagide is a class of iridoid glycoside isolated from Scrophularia ningpoensis and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes (*T.b. rhodesiense) with an IC₅₀* of 21 μg/mL. Harpagide exerts significant antileishmanial activity against *L. donovani* with an IC₅₀ value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities.

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