ChemicalBook > CAS DataBase List > 1358099-18-9

1358099-18-9

Product Name
1358099-18-9
CAS No.
1358099-18-9
Chemical Name
1358099-18-9
Synonyms
C25-140, 10 mM in DMSO;TRAF6-UBC13 INHIBITOR C25-140;1-(4-benzylpiperidin-1-yl)-3-(3,5-dimethyl-1-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl)propan-1-one;1-Propanone, 3-[3,5-dimethyl-1-(3-methyl-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl]-1-[4-(phenylmethyl)-1-piperidinyl]-;1-(4-Benzylpiperidin-1-yl)-3-(3,5-dimethyl-1-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl)propan-1-one , C25-140;Ubiquitin conjugating enzyme,Ubiquitin ligase,Ubiquitin activating enzyme,C25 140,TNF Receptor,E3 ligating enzyme,C-25-140,E1/E2/E3 Enzyme,C25-140,C25140,Tumor Necrosis Factor Receptor,E2 conjugating enzyme,E1 activating enzyme,TNFR,inhibit,Inhibitor
CBNumber
CB14815436
Molecular Formula
C26H31N7O
Formula Weight
457.57
MOL File
1358099-18-9.mol
More
Less

1358099-18-9 Property

Density 
1.29±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:62.5(Max Conc. mg/mL);136.59(Max Conc. mM)
form 
Solid
pka
-0.22±0.30(Predicted)
color 
White to off-white
More
Less

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..…

More
Less

N-Bromosuccinimide Price

ChemScene
Product number
CS-0079668
Product name
C25-140
Purity
99.84%
Packaging
5mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-0079668
Product name
C25-140
Purity
99.84%
Packaging
10mg
Price
$280
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
INB0009817
Product name
C25-140
Purity
95.00%
Packaging
5MG
Price
$455.68
Updated
2021/12/16
ChemScene
Product number
CS-0079668
Product name
C25-140
Purity
99.84%
Packaging
50mg
Price
$990
Updated
2021/12/16
ChemScene
Product number
CS-0079668
Product name
C25-140
Purity
99.84%
Packaging
100mg
Price
$1700
Updated
2021/12/16
More
Less

1358099-18-9 Chemical Properties,Usage,Production

Uses

C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity[1].

in vivo

C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in R 837-induced psoriasis mouse model[1].
C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model[1].
C25-140 (10 mg/kg; i.v.) treatment shows that the Cmax, AUC, t1/2 and Vd are 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively[1].
C25-140 (10 mg/kg; p.o.) treatment shows that the Cmax, AUC, t1/2 and Vd are 3.4 μg/mL, 124034 ng min/mL, 127.33 min and 13.3 L/kg, respectively[1].
C25-140 (10 mg/kg; i.p.) treatment shows that the Cmax, AUC, t1/2 and Vd are 4.2μg/mL, 100000 ng min/mL, 184 min, 25.6 L/kg, respectively[1].

Animal Model:R 837-induced psoriasis mouse model (male BALB/c mice)[1]
Dosage:~1.5 mg/kg
Administration:Topically to the shaved back and the right ear; twice daily for 6 days
Result:Showed a dose-dependent improvement of RA disease outcome.
Animal Model:Collagen-induced arthritis (CIA) model in DBA1/J mice[1]
Dosage:6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:Given i.p.; twice daily for 14 days
Result:Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.
Animal Model:BALB/C mice[1]
Dosage:10 mg/kg
Administration:I.v. (Pharmacokinetic Analysis)
Result:The Cmax, AUC, t1/2 and Vd were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.

storage

Store at -20°C

References

[1] Brenke JK, et al. Targeting TRAF6 E3 ligase activity with a small-molecule inhibitor combats autoimmunity. J Biol Chem. 2018 Aug 24;293(34):13191-13203. DOI:10.1074/jbc.RA118.002649

1358099-18-9 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

1358099-18-9 Suppliers

China 48 United States 5 Global 53
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
EnliPharma Technology Co., Ltd
Tel
0551-66399836 18955197623
Email
sales@enlipharma.com
Country
China
ProdList
1876
Advantage
55
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4827
Advantage
55
Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Fax
QQ: 12922499
Email
huahero21@sina.com
Country
China
ProdList
2586
Advantage
55
Artis Biotech Co. Ltd.
Tel
19138486554; 18108108965
Fax
0575-89298961
Email
sales@artisbio.com
Country
China
ProdList
2333
Advantage
58
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
86249
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
7999
Advantage
62
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 18101056239
Email
3193328036@qq.com
Country
China
ProdList
29661
Advantage
68
Heze Development Zone chuangli Chemical Co., Ltd.
Tel
0530-+86-530-529 6766，+86-15666160102 15666160102
Fax
0530-529 6766
Email
info@chuangli-chem.com
Country
China
ProdList
852
Advantage
55

1358099-18-9, 1358099-18-9Related Search:


  • 1-(4-benzylpiperidin-1-yl)-3-(3,5-dimethyl-1-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl)propan-1-one
  • TRAF6-UBC13 INHIBITOR C25-140
  • 1-Propanone, 3-[3,5-dimethyl-1-(3-methyl-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl]-1-[4-(phenylmethyl)-1-piperidinyl]-
  • Ubiquitin conjugating enzyme,Ubiquitin ligase,Ubiquitin activating enzyme,C25 140,TNF Receptor,E3 ligating enzyme,C-25-140,E1/E2/E3 Enzyme,C25-140,C25140,Tumor Necrosis Factor Receptor,E2 conjugating enzyme,E1 activating enzyme,TNFR,inhibit,Inhibitor
  • 1-(4-Benzylpiperidin-1-yl)-3-(3,5-dimethyl-1-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazol-4-yl)propan-1-one , C25-140
  • C25-140, 10 mM in DMSO
  • 1358099-18-9