SML2183
LY2955303
≥98% (HPLC)
Synonym(s):
4-[5-[3,5-bis(1,1-Dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]-benzoic acid, LY 2955303
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| Pack Size | SKU | Availability | Price |
|---|---|---|---|
| 25 mg | Please contact Customer Service for Availability | PLN 1,480.00 |
About This Item
Empirical Formula (Hill Notation):
C36H42N4O3
CAS Number:
Molecular Weight:
578.74
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC(C)(C)C1=CC(C2=CC(C3=CC=C(C(O)=O)C=C3)=NN2C4=CC=C(C=C4)C(N5CCN(CC5)C)=O)=CC(C(C)(C)C)=C1
InChI key
YVXYHNKIOFSFMZ-UHFFFAOYSA-N
Biochem/physiol Actions
LY2955303 is a potent and selective RARγ antagonist (Ki = 1.09 nM/RARγ, >1.70 μM/RARα, >2.98 μM/RARβ) that 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/RARγ, 1.51 μM/RARβ, 4.44 μM/RARα; 10 nM ATRA for RARβ transfectant). LY2955303 exhibits therapeutic efficacy in a rat 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 properties, aqueous 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.
Potent and selective retinoic acid receptor gamma (RARγ) antagonist with oral availability and in vivo efficacy in a rat model of osteoarthritis-like joint pain.
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This Item | |||
|---|---|---|---|
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| form powder | form powder | form powder | form powder |
| storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C |
| solubility DMSO: 2 mg/mL, clear | solubility DMSO: 2 mg/mL, clear | solubility DMSO: 20 mg/mL, clear | solubility DMSO: 2 mg/mL, clear |
| color white to beige | color white to beige | color white to beige | color white to beige |
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Norman E Hughes et al.
Bioorganic & medicinal chemistry letters, 26(14), 3274-3277 (2016-06-05)
A series of triaryl pyrazoles were identified as potent pan antagonists for the retinoic acid receptors (RARs) α, β and γ. X-ray crystallography and structure-based drug design were used to improve selectivity for RARγ by targeting residue differences in the
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML2183-5MG | 04061835503391 |
| SML2183-25MG | 04061835503407 |