1206880-66-1
1206880-66-1 structure
- Name: AM679
- Chemical Name: 3-[5-[[(2S)-1-acetyl-2,3-dihydroindol-2-yl]methoxy]-3-tert-butylsulfanyl-1-[[4-(5-methoxypyrimidin-2-yl)phenyl]methyl]indol-2-yl]-2,2-dimethylpropanoic acid
- CAS Number: 1206880-66-1
- Molecular Formula: C40H44N4O5S
- Molecular Weight: 692.86600
- Catalog: Signaling Pathways Immunology/Inflammation FLAP
- Create Date: 2016-08-23 12:04:17
- Modify Date: 2024-01-06 13:33:31
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AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1]Target: FLAPin vitro: AM679 showed excellent in vitro inhibition against FLAP. AM679 has an excellent hWB IC50 potency of 154 nM. AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10 uM) and no CYP3A4 induction.in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production ofleukotrienes in vivo.16 Oral administration of 39 (10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM).
| Name | 3-[5-[[(2S)-1-acetyl-2,3-dihydroindol-2-yl]methoxy]-3-tert-butylsulfanyl-1-[[4-(5-methoxypyrimidin-2-yl)phenyl]methyl]indol-2-yl]-2,2-dimethylpropanoic acid |
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| Synonyms |
UNII-65KJ8P7M9D
AM-679 3-{5-((S)-N-acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid CS-0935 AM679||AM 679 AM679 |
| Description | AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1]Target: FLAPin vitro: AM679 showed excellent in vitro inhibition against FLAP. AM679 has an excellent hWB IC50 potency of 154 nM. AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10 uM) and no CYP3A4 induction.in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production ofleukotrienes in vivo.16 Oral administration of 39 (10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM). |
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| Related Catalog | |
| References |
| Molecular Formula | C40H44N4O5S |
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| Molecular Weight | 692.86600 |
| Exact Mass | 692.30300 |
| PSA | 132.08000 |
| LogP | 8.12070 |
| Storage condition | 2-8℃ |