Fig. 1 · Structure

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Nitisinone

Cat. No. A11093 CAS 104206-65-7

HPPD inhibitor

Nitrisinone is a competitive inhibitor that reversibly inhibits 4-Hydroxyphenylpyruvate oxidase (dioxygenase).

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In Vivo Studies

Approximately 90% of male Glossina pallidipes died after 26 hours of feeding on Wistar rats receiving oral Nitisinone at 1 mg/kg. In G. m. morsitans, comparison of horse blood supplemented with Nitisinone or PBS yielded an LC50 = 2.07 μM for Nitisinone, which was approximately 173 times more potent than mesotrione. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Fly survival after feeding on treated rats

Animal study · Male Glossina pallidipes; Wistar rats [1]

Male Glossina pallidipes fed on Wistar rats receiving Nitisinone at 1 mg/kg by oral gavage in sterile PBS. After 26 hours of feeding, approximately 90% of the flies died.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Male Glossina pallidipes survivalfly mortality approximately 90% of the flies died[1]

Conditions shared by the study groups

Route
oral dose of NTBC solubilised in sterile PBS by gavage
Treatment course
After 90 minutes; after 26 hours of feeding
Vehicle
sterile PBS
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Nitisinone 1 mg/kgPBS-treated anaesthetized ratsafter 26 hours of feeding on rats receiving an oral dose of NTBC equal to 1 mg/kg (therapeutic dose recommended for humans with HT- I), approximately 90% of the flies died[1]
Nitisinone 1 mg/kg
Model: Male Glossina pallidipes; Wistar rats
Methods and source locations

Compound reported in the paper: Nitisinone; Compound label in the paper: NTBC

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Tsetse fed on NTBC-treated mice die (S21); Materials and methods > Ethics statement (S86); Materials and methods > In vivo oral administration of NTBC to rats (S172, S174, S176); Fig 1 legend (S266)

Male Glossina pallidipes survival: Male Glossina pallidipes survival; comparator: PBS-treated anaesthetized rats — Results > Tsetse fed on NTBC-treated mice die (S21); Fig 1 legend (S266)

Nitisinone 1 mg/kg · Results > Tsetse fed on NTBC-treated mice die (S21); Materials and methods > In vivo oral administration of NTBC to rats (S172, S174)

Survival of tsetse flies following treated bloodmeals

Animal study · G. m. morsitans [1]

G. m. morsitans received artificial bloodmeals containing horse blood supplemented with Nitisinone or PBS. In this comparison, Nitisinone had an LC50 = 2.07 μM and was approximately 173 times more potent than mesotrione.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
survival 24 hours PBMLC50 LC50 = 2.07 μM[1]

Conditions shared by the study groups

Route
fed to tsetse flies in an artificial bloodmeal
Treatment course
24 hours PBM
Vehicle
sterile PBS
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Nitisinone 0.05, 0.025, 0.01, 0.005, 0.0025, 0.00075, 0.0005, 0.00025, and 0.0001 mg/mlPBS (Controlapproximately 173 times more potent than mesotrione with a LC50 = 2.07 μM[1]
Nitisinone 0.05, 0.025, 0.01, 0.005, 0.0025, 0.00075, 0.0005, 0.00025, and 0.0001 mg/ml
Model: G. m. morsitans
Methods and source locations

Compound reported in the paper: Nitisinone; Compound label in the paper: NTBC

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Ingestion of NTBC is lethal to tsetse (S14); Materials and methods > Oral dosing of mesotrione and NTBC (S139, S140, S143); Fig 1 legend (S261, S265)

survival 24 hours PBM: survival 24 hours PBM; comparator: PBS (Control — Results > Ingestion of NTBC is lethal to tsetse (S14); Fig 1 legend (S265)

Nitisinone 0.05, 0.025, 0.01, 0.005, 0.0025, 0.00075, 0.0005, 0.00025, and 0.0001 mg/ml · Results > Ingestion of NTBC is lethal to tsetse (S14); Materials and methods > Oral dosing of mesotrione and NTBC (S143); Fig 1 legend (S265)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 104206-65-7
Applications HPPD inhibitor
Formula C14H10F3NO5
Molecular Weight 329.2
Synonyms SC 0735; NTBC
SMILES
C1CC(=O)C(C(=O)C1)C(=O)C2=C(C=C(C=C2)C(F)(F)F)[N+](=O)[O-]

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 62 mg/mL (188.32 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Sterkel M, Haines LR, Casas-Sánchez A, et al. Repurposing the orphan drug nitisinone to control the transmission of African trypanosomiasis. PLoS Biol (2021). PMID: 33497373 DOI: 10.1371/journal.pbio.3000796 Source material

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