| Identification | Back Directory | [Name]
IN 1130 | [CAS]
868612-83-3 | [Synonyms]
IN 1130
IN1130,IN 1130
3-[[5-(6-Methyl-2-pyridinyl)-4-(6-quinoxalinyl)-1H-imidazol-2-yl]methyl]benzamide | [Molecular Formula]
C25H20N6O | [MDL Number]
MFCD19441274 | [MOL File]
868612-83-3.mol | [Molecular Weight]
420.47 |
| Chemical Properties | Back Directory | [Boiling point ]
705.6±60.0 °C(Predicted) | [density ]
1.315±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
9.60±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
IN 1130 is a novel transforming growth factor-?β type I receptor kinase (ALK5) inhibtior. In one study, it showed that IN-1130 was effective in prevention and treatment of renal fibrosis in rat unilateral ureteral obstruction model. | [Biological Activity]
IN-1130 is a potent inhibitor of the activin receptor-like kinase ALK-5 (Type 1 TGF1β recptor). The compound inhibits phosphorylation of Smad-2 with an IC50 of 36 nM. IN-1130 inhibits renal fibrosisand also reduces tumor volume in prostate tumor xenografts in murine models. | [in vivo]
IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats[1].
?
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys[1].
?
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].
| Animal Model: | Six-week-old male Sprague–Dawley rats weighing 180-200 g[1] | | Dosage: | 10 and 20 mg/kg | | Administration: | IP; daily; for 7 and 14 days | | Result: | Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.
|
| [IC 50]
ALK5 | [storage]
Store at -20°C |
|
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
R&D Systems, Inc
|
| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
|