Bulk Inquiry
LY 2955303 dihydrochloride
- Parent CAS: 1433497-19-8
- Soluble in DMSO
- MF: C36H42N4O3.2HCl
- MW: 651.67
Description
LY 2955303 dihydrochloride is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a binding affinity (Ki) of 1.1 nM. It demonstrates >500-fold selectivity over both RARα (Ki > 1,700 nM) and RARβ (Ki > 2,980). In cellular models, it fully blocks RARγ-dependent reporter gene expression stimulated by all-trans retinoic acid (ATRA) without interfering with alpha or beta pathways.
RARγ pharmacology is highly relevant to arthritic disease and pain pathways. As a selective chemical tool, LY 2955303 dihydrochloride supports mechanistic studies of RARγ and NR1B nuclear receptor signaling across biochemical, cellular, and translational disease-model assays.
Key Features
- Highly potent and selective RARγ antagonist
- Ki 1.1 nM for RARγ, >500-fold selective over RARα and RARβ
- Modulates RARγ-dependent biological activity
- Prove for RARγ pathway studies
Applications
- RARγ pharmacology and target-validation studies
- Disease-model research related to arthritis, pain
- Treatment of osteoarthritis joint pain
More Information
| Parent CAS No. | 1433497-19-8 |
|---|---|
| Chemical Name | 4-(5-(3,5-ditert-butylphenyl)-1-(4-(4-methylpiperazine-1-carbonyl)phenyl)-1H-pyrazol-3-yl)benzoic acid dihydrochloride |
| SMILES | C(O)(=O)C1=CC=C(C2C=C(C3=CC(C(C)(C)C)=CC(C(C)(C)C)=C3)N(C3=CC=C(C(N4CCN(C)CC4)=O)C=C3)N=2)C=C1.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C36H42N4O3.2ClH/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);2*1H |
| InChiKey | ZPIGNDDTRHLVIS-UHFFFAOYSA-N |
| CID | 134824562 |
| Short Description | RARγ antagonist |
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1173 | BMS 270394 |
From $181.50 |
| 1194 | BMS 189961 |
From $159.50 |
| 1241 | CH 55 |
From $99.00 |
| 1242 | LE 135 |
From $132.00 |
| 1700 | Bexarotene |
From $71.50 |
| 2408 | NRX 194204 |
From $132.00 |
| 2679 | AR7 |
From $99.00 |
| 2902 | QX77 |
From $132.00 |
| 2948 | AM 580 |
From $110.00 |
| 3321 | Retinoic acid |
From $55.00 |
