| Identification | Back Directory | [Name]
Firategrast | [CAS]
402567-16-2 | [Synonyms]
CS-1588
SB683699
SB-683699
SB 683699
402567-16-2
Firategrast
SB-683699; SB683699
SB-683699，Firategrast
Firategrast (SB 683699)
SB-683699;SB 683699;SB683699
(S)-2-(2,6-difluorobenzamido)-3-(4'-(ethoxymethyl)-2',6'-dimethoxy-[1,1'-biphenyl]-4-yl)propanoic acid
[1,1'-Biphenyl]-4-propanoic acid, α-[(2,6-difluorobenzoyl)aMino]-4'-(ethoxyMethyl)-2',6'-diMethoxy-, (αS)-
(alphaS)-alpha-[(2,6-Difluorobenzoyl)amino]-4'-(ethoxymethyl)-2',6'-dimethoxy-[1,1'-biphenyl]-4-propanoic acid | [Molecular Formula]
C27H27F2NO6 | [MOL File]
402567-16-2.mol | [Molecular Weight]
499.5 |
| Chemical Properties | Back Directory | [Melting point ]
154-155℃ (ethanol water ) | [Boiling point ]
594.4±50.0 °C(Predicted) | [density ]
1.261±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥50 mg/mL in DMSO; insoluble in H2O; ≥90.8 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
3.51±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Treatment of multiple sclerosis and inflammatory bowel disease. | [Biological Activity]
Firategrast is an orally availablepotent and selective antagonist of α4β1/α4β7 integrins. Firategrast inhibits α4β1/α4β7 integrin-mediated transferring of lymphocytes into the central nervous system (CNS). In phase II trial it demonstrated a reduction of new contrast enhancing MRI lesions in patients with relapsing remitting MS. | [in vivo]
Firategrast (30?mg/kg/day in drinking water; starting 2 or 7 days post transplantation to 21 days) shows an overall reduction of leukemic cells in the spleen[3].
| Animal Model: | Female Wild-type C57BL/6J mice (8-12 weeks) with primary TCL1-tg splenocytes[3] | | Dosage: | 30?mg/kg | | Administration: | Drinking water; daily; starting 2 or 7 days post transplantation to 21 days | | Result: | Showed an overall reduction of leukemic cells in the spleen, accompanied by significant spleen weight reduction.
|
| [target]
α4β1/α4β7 integrin | [IC 50]
α4β1; α4β7 | [storage]
Store at -20°C |
|
| Company Name: |
Cool Pharm, Ltd
|
| Tel: |
021-58581007 18019463053 |
| Website: |
http://www.coolpharm.com |
|