DDD85646
- Product Name
- DDD85646
- CAS No.
- 1215010-55-1
- Chemical Name
- DDD85646
- Synonyms
- DDD85646;DDD 85646 (DDD85646);DDD85646 Hydrochloride;DDD85646, 10 mM in DMSO;2,6-Dichloro-4-(2-(piperazin-1-yl)pyridin-4-yl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide;2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide;Benzenesulfonamide, 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-;2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzene-1-sulfonamide;African trypanosomiasis,N-myristoyltransferase,inhibit,DDD85646,Inhibitor,trypanosoma brucei,DNA/RNA Synthesis,NMT,Parasite
- CBNumber
- CB34666388
- Molecular Formula
- C21H24Cl2N6O2S
- Formula Weight
- 495.43
- MOL File
- 1215010-55-1.mol
DDD85646 Property
- 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)
- pka
- 7.04±0.50(Predicted)
- form
- Solid
- color
- Off-White to Yellow
N-Bromosuccinimide Price
- Product number
- 13839
- Product name
- DDD85646
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $97
- Updated
- 2024/03/01
- Product number
- 13839
- Product name
- DDD85646
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $410
- Updated
- 2024/03/01
- Product number
- 13839
- Product name
- DDD85646
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $672
- Updated
- 2024/03/01
- Product number
- D195323
- Product name
- DDD85646
- Packaging
- 2.5mg
- Price
- $265
- Updated
- 2021/12/16
- Product number
- 445831
- Product name
- DDD85646
- Packaging
- 1mg
- Price
- $410
- Updated
- 2021/12/16
DDD85646 Chemical Properties,Usage,Production
Description
DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki 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
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
DDD85646 Preparation Products And Raw materials
Raw materials
Preparation Products
DDD85646 Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- tp@aladdinsci.com
- Country
- United States
- ProdList
- 52924
- Advantage
- 58
- Tel
- --
- Fax
- --
- cayman@caymanchem.com
- Country
- United States
- ProdList
- 6213
- Advantage
- 81