ChemicalBook CAS DataBase List 1215010-55-1

1215010-55-1

Name	DDD85646
CAS	1215010-55-1
Molecular Formula	C21H24Cl2N6O2S
Molecular Weight	495.43
MOL File	1215010-55-1.mol

Chemical Properties

Melting point	>215°C (dec.)
Boiling point	684.3±65.0 °C(Predicted)
density	1.48±0.1 g/cm3(Predicted)
storage temp.	Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility	DMSO (Slightly, Heated), Methanol (Slightly)
form	Solid
pka	7.04±0.50(Predicted)
color	Off-White to Yellow

Hazard Information

Description

DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent K_i value of 1.44 nM. T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT. It less potently inhibits growth of T. cruzi (EC₅₀ = 6.9 μM).

Uses

DDD85646 is a potent inhibitor of Trypanosoma brucei N-myristoyltransferase (TbNMT).

in vivo

DDD85646 (10, 50 mg/kg; Oral administration; 1) has moderate bioavailability (about 20%) in female NMRI mouse models, and the free drug level is higher than EC₉₉ (EC₉₉ is about 6 nM), which can effectively inhibit the proliferation of T. b. brucei^[3].
DDD85646 (0-50 mg/kg; Oral administration; Twice a day; 4 days) kills Trypanosoma brucei by acting on TbNMT in T. b. brucei acute mouse model of HAT^[3].
DDD85646 (50 mg/kg; Oral administration; Twice a day) shows significant antitrypanosomic activity in female NMRI mice models^[3].

Animal Model:	T. b. brucei acute mouse model of HAT^[3]
Dosage:	0-50 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Cured all animals in the T. b. brucei acute mouse model of HAT at a minimal oral dose of 12.5 mg/kg (b.i.d. for 4 days) Prevented 99% of T. b. brucei proliferation Parasite numbers dropped below detectable levels within 12 hours

IC 50

Trypanosoma

storage

Store at -20°C

References

[1] JULIE A. FREARSON. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness[J]. Nature, 2010, 464 7289: 728-732. DOI: 10.1038/nature08893

Spectrum Detail

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