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
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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
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Hazard and Precautionary Statements (GHS)

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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
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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

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1358099-18-9 Suppliers

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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