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Purity: ≥98%
LY2955303 (LY-2955303) is a novel, potent and selective antagonist of retinoic acid receptor gamma (RARγ) with potential to manage osteoarthritis pain. It inhibits RARγ with a Ki of 1.09 nM. LY2955303 has the potential for the treatment of osteoarthritis pain. LY2955303 demonstrated good pharmacokinetic properties and was efficacious in the MIA model of osteoarthritis-like joint pain. LY2955303 demonstrated an improved margin to RAR -mediated adverse effects.
| ln Vitro |
In tests, it was found that LY2955303 bound RARα, RARβ, and RARγ with Ki values of >1700, >2980, and 1.09 nM, respectively. RARγ has a functioning Ki of 7.1±4.9 nM[1].
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| ln Vivo |
A dose-response impact was demonstrated by the single-shot barrier LY2955303, and the weight-bearing variance (ED50=0.72 mg/kg) was decreased by the trap [1].
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| References |
[1]. Hughes NE, et al. Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277.
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| Molecular Formula |
C36H42N4O3
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|---|---|
| Molecular Weight |
578.743689060211
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| CAS # |
1433497-19-8
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| SMILES |
O=C(O)C1=CC=C(C2=NN(C3=CC=C(C(N4CCN(C)CC4)=O)C=C3)C(C5=CC(C(C)(C)C)=CC(C(C)(C)C)=C5)=C2)C=C1
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| InChi Key |
YVXYHNKIOFSFMZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C36H42N4O3/c1-35(2,3)28-20-27(21-29(22-28)36(4,5)6)32-23-31(24-8-10-26(11-9-24)34(42)43)37-40(32)30-14-12-25(13-15-30)33(41)39-18-16-38(7)17-19-39/h8-15,20-23H,16-19H2,1-7H3,(H,42,43)
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| Chemical Name |
4-(5-(3,5-di-tert-butylphenyl)-1-(4-(4-methylpiperazine-1-carbonyl)phenyl)-1H-pyrazol-3-yl)benzoic acid
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| Synonyms |
LY-2955303; LY2955303; LY 2955303.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~30 mg/mL (~51.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7279 mL | 8.6395 mL | 17.2789 mL | |
| 5 mM | 0.3456 mL | 1.7279 mL | 3.4558 mL | |
| 10 mM | 0.1728 mL | 0.8639 mL | 1.7279 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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