Basic information Safety Supplier Related

LY-2562175

Basic information Safety Supplier Related

LY-2562175 Basic information

Product Name:
LY-2562175
Synonyms:
  • LY-2562175
  • CS-2847
  • 1H-Indole-3-carboxylic acid, 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]-1-piperidinyl]-1-methyl-
  • LY 2562175,NR1H4,Inhibitor,LY-2562175,Autophagy,LY2562175,inhibit,FXR
  • 6-(4-((5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic acid
  • LY2562175, 10 mM in DMSO
  • TERN-101
CAS:
1103500-20-4
MF:
C28H27Cl2N3O4
MW:
540.44
Mol File:
1103500-20-4.mol
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LY-2562175 Chemical Properties

Boiling point:
740.1±60.0 °C(Predicted)
Density 
1.48±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 20 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
form 
A crystalline solid
pka
3.43±0.10(Predicted)
color 
White to light yellow
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LY-2562175 Usage And Synthesis

Description

LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay). It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC50s = >10 μM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC50 value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.

Uses

LY2562175, is a potent and selective FXR agonist with an EC50 of 193 nM.

in vivo

LY2562175 causes a dose-dependent decrease in serum cholesterol and serum triglycerides. At a dose of 10 mg/kg, the decrease in cholesterol with LY2562175 is 80% below vehicle-treated animals, and the decrease in serum triglycerides is 76% from control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. Treatment of female ZDF rats with LY2562175 results in a dose dependent lowering of plasma triglycerides in the fasted and nonfasted states. When administered as a fixed dose combination with BRL49653, LY2562175 further lowers fasted and nonfasted plasma triglycerides. FPLC fractionation of the lipoproteins reveals that LY2562175 treatment results in a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model[1].

LY-2562175Supplier

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