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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
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
- 021-52996696,15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4817
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 86249
- Advantage
- 60
- Tel
- 021-QQ:65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9505
- Advantage
- 58
- Tel
- 400-9205774
- sales@glpbio.cn
- Country
- China
- ProdList
- 6777
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32467
- Advantage
- 58
- Tel
- 0512-13601744364 13601744364
- chemsharker@126.com
- Country
- China
- ProdList
- 1139
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 4887
- Advantage
- 58
- Tel
- 15921930842 15921930842
- yh-wang@univ-bio.com
- Country
- China
- ProdList
- 25004
- Advantage
- 58