| Identification | Back Directory | [Name]
Etalocib | [CAS]
161172-51-6 | [Synonyms]
VML 295
Etalocib
LY293111
LY293111 Exclusive
YFIZRWPXUYFCSN-UHFFFAOYSA-N
Benzoic acid, 2-[3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-2-propylphenoxy]- | [Molecular Formula]
C33H33FO6 | [MDL Number]
MFCD11977723 | [MOL File]
161172-51-6.mol | [Molecular Weight]
544.61 |
| Chemical Properties | Back Directory | [Melting point ]
68-70 °C(Solv: acetonitrile (75-05-8)) | [Boiling point ]
656.8±55.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:98.5(Max Conc. mg/mL);173.85(Max Conc. mM) | [form ]
Solid | [pka]
3.32±0.36(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Antineoplastic (inhibits formation of 5-LO, LTB4,LTC4, and thromboxane B2(TxB2); activates PPARγ nuclear receptors). | [Definition]
ChEBI: LY293111 is an aromatic ether. | [in vivo]
Etalocib produces a dose-related inhibition of acute leukotriene B4-induced airway obstruction when administered i.v. (ED50=14 μg/kg) or p.o. (ED50=0.4 mg/kg)[2].
Etalocib (10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h[2].
Etalocib (250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice[3].
| Animal Model: | Guinea pigs[2].
| | Dosage: | 1-10 mg/kg. | | Administration: | Orally once. | | Result: | A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge.
Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge.
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| [IC 50]
LTB4 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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