ChemicalBook > CAS DataBase List > DDD85646

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
More
Less

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
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

N-Bromosuccinimide Price

Cayman Chemical
Product number
13839
Product name
DDD85646
Purity
≥98%
Packaging
1mg
Price
$97
Updated
2024/03/01
Cayman Chemical
Product number
13839
Product name
DDD85646
Purity
≥98%
Packaging
5mg
Price
$410
Updated
2024/03/01
Cayman Chemical
Product number
13839
Product name
DDD85646
Purity
≥98%
Packaging
10mg
Price
$672
Updated
2024/03/01
TRC
Product number
D195323
Product name
DDD85646
Packaging
2.5mg
Price
$265
Updated
2021/12/16
Usbiological
Product number
445831
Product name
DDD85646
Packaging
1mg
Price
$410
Updated
2021/12/16
More
Less

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

More
Less

DDD85646 Suppliers

Bide Pharmatech Ltd.
Tel
400-164-7117 13681763483
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
42446
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4762
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9079
Advantage
58
Shanghai Hongye Biotechnology Co. Ltd
Tel
400-9205774
Email
sales@glpbio.cn
Country
China
ProdList
6777
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
Shanghai Dongyang Biotechnology Co., Ltd.
Tel
0512-0512-13601744364 13601744364
Email
chemsharker@126.com
Country
China
ProdList
1010
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
Email
3525679403@qq.com
Country
China
ProdList
4989
Advantage
58

1215010-55-1, DDD85646Related Search:


  • DDD85646
  • DDD 85646 (DDD85646)
  • Benzenesulfonamide, 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-
  • DDD85646 Hydrochloride
  • African trypanosomiasis,N-myristoyltransferase,inhibit,DDD85646,Inhibitor,trypanosoma brucei,DNA/RNA Synthesis,NMT,Parasite
  • 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide
  • 2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzene-1-sulfonamide
  • 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
  • 1215010-55-1
  • C21H24Cl2N6O2S