| Company Name: |
TargetMol Chemicals Inc.
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15002134094 |
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| Products Intro: |
Product Name:Hedgehog IN-5
CAS:1544681-93-7
Package:50mg;10mg
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| | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- Basic information |
| Product Name: | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- | | Synonyms: | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel-;Hedgehog IN-5 | | CAS: | 1544681-93-7 | | MF: | C27H31ClF3N5O | | MW: | 534.02 | | EINECS: | | | Product Categories: | | | Mol File: | 1544681-93-7.mol | ![Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- Structure](CAS/20210305/GIF/1544681-93-7.gif) |
| | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- Chemical Properties |
| Boiling point | 617.9±55.0 °C(Predicted) | | density | 1.259±0.06 g/cm3(Predicted) | | pka | 11.84±0.70(Predicted) |
| | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- Usage And Synthesis |
| Uses | Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease[1]. | | in vivo | Modeling methods: Bleomycin (HY-108345) (3 mg/kg; Intratracheal injection for 8 days)-induced pulmonary fibrosis model in rats.
Hedgehog IN-5 (5-30 mg/kg; Oral administration after 8 days of moulding; once daily for 2 weeks) inhibits the progression of pulmonary fibrosis induced by Bleomycin (HY-108345) in several pathological evaluation indexes in SD rat model of unilateral pulmonary fibrosis, significantly[1].
Modeling methods: CCL4 (dissolved in olive oil at a dose of 0.5 μL/g; Oral administration; Three times a week for four weeks)-induced liver fibrosis model in C57BL/6 mice.
Hedgehog IN-5 (5-20 mg/kg; Oral administration on the day of moulding; Once a day for 4 weeks) exhibits a certain trend of inhibiting CCl4-induced liver fibrosis. And primarily manifests as a reduction in hepatocyte degeneration and necrosis, as well as a decrease in fibrotic area in CCL4-induced liver fibrosis model in C57BL/6 mice[1].
Hedgehog IN-5 (10-20 mg/kg, 20mg/kg (Combined with BIBF1120 (50 mg/kg); Oral administration; Once a day for 20 days) alone or in combination with BIBF1120 significantly inhibits bleomycin-induced lung tissue inflammation and fibrosis[1]. | Animal Model: | Unilateral pulmonary fibrosis in SD rat model[1] | | Dosage: | 5 mg/kg, 15 mg/kg, 30 mg/kg | | Administration: | Oral administration after 8 days of moulding; once daily for 2 weeks | | Result: | Reduced the scores of Bleomycin (HY-108345)-treated mice, significantly.
Collagen content in the lungs as well as myofibroblasts were quantified to assess the antifibrotic effect of Hedgehog IN-5, α-SMA protein percentage was significantly reduced with 30 mg/kg dose and collagen content was not significantly changed. |
| Animal Model: | CCL4-induced liver fibrosis model in C57BL/6 mice[1] | | Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg | | Administration: | Oral administration on the day of moulding; Once a day for four weeks | | Result: | Showed slow weight gain after one week and no significant weight gain after two weeks at the dose of 20 mg/kg.
Serum biochemical detection in peripheral blood showed that ALT and AST were significantly reduced but TBIL had no change at the dose of 20mg/kg.
Liver histopathological analysis showed that the liver injury score decreased and the fibrosis area of liver tissue decreased.
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| | References | [1] Cai, Sui Xiong et al. Application of hedgehog pathway inhibitor for treatment of fibrotic diseases. World Intellectual Property Organization, WO2018082587 A1 2018-05-11 |
| | Benzamide, N-[4-chloro-3-[5-(1-methylethyl)-1H-imidazol-2-yl]phenyl]-2-(trifluoromethyl)-4-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- Preparation Products And Raw materials |
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