| Identification | Back Directory | [Name]
LY2955303 | [CAS]
1433497-19-8 | [Synonyms]
CS-2631
LY2955303
LY2955303 >=98% (HPLC)
LY2955303; LY-2955303; LY 2955303
4-[5-[3,5-Bis(1,1-dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]benzoic acid
Benzoic acid, 4-[5-[3,5-bis(1,1-dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]- | [Molecular Formula]
C36H42N4O3 | [MOL File]
1433497-19-8.mol | [Molecular Weight]
578.74 |
| Chemical Properties | Back Directory | [Boiling point ]
721.9±60.0 °C(Predicted) | [density ]
1.15±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
Chloroform: 25 mg/ml | [form ]
A crystalline solid | [pka]
3.84±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
LY 2955303, is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM. | [Biological Activity]
LY2955303 is a potent and selective RARγ antagonist (Ki = 1.09 nM/RARγ>1.70 μM/RARα>2.98 μM/RARβ) th at effectively inhibits RARγ-but not RARα- or RARβ-dependent reporter activity upon 15 nM all-trans retinoic acid stimulation in respective HEK293 transfectants (KB = 7.11 nM/RARγ1.51 μM/RARβ4.44 μM/RARα; 10 nM ATRA for RARβ transfectant). LY2955303 exhibits therapeutic efficacy in a r at model of osteoarthritis-like joint pain (ED50 = 0.72 mg/kg; single p.o. dosage 9 days post OA pain induction by MIA intra-articular injection) with good pharmacokinetic propertiesaqueous solubility (>1.0 mg/mL in simulated intestinal fluid)oral availability (F = 26%; 10 mg/kg p.o. over 2 mg/kg i.v.)and no RARα antagonism-associated adverse effects (no testicular degeneration up to 10 mg/kg) seen with BMS-189453 treatment or in RARα-knockout mice. | [storage]
Store at -20°C |
|
| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
http://m.is0513.com/ShowSupplierProductsList15061/0.htm |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
http://m.is0513.com/ShowSupplierProductsList927327/0.htm |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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