LY-2562175

Product Name: LY-2562175
CAS No.: 1103500-20-4
Chemical Name: LY-2562175
Synonyms: CS-2847;TERN-101;LY-2562175;LY2562175, 10 mM in DMSO;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;1H-Indole-3-carboxylic acid, 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]-1-piperidinyl]-1-methyl-
CBNumber: CB83303953
Molecular Formula: C28H27Cl2N3O4
Formula Weight: 540.44
MOL File: 1103500-20-4.mol

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LY-2562175 Property

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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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 28912
Product name: LY2562175
Packaging: 10mg
Price: $1116
Updated: 2024/03/01

Cayman Chemical

Product number: 28912
Product name: LY2562175
Packaging: 25mg
Price: $1918
Updated: 2024/03/01

Cayman Chemical

Product number: 28912
Product name: LY2562175
Packaging: 1mg
Price: $141
Updated: 2024/03/01

Cayman Chemical

Product number: 28912
Product name: LY2562175
Packaging: 5mg
Price: $594
Updated: 2024/03/01

TRC

Product number: L490015
Product name: LY2562175
Packaging: 10mg
Price: $1135
Updated: 2021/12/16

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LY-2562175 Chemical Properties,Usage,Production

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].

References

[1] MICHAEL J. GENIN*. Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia[J]. Journal of Medicinal Chemistry, 2015, 58 24: 9768-9772. DOI: 10.1021/acs.jmedchem.5b01161

LY-2562175 Preparation Products And Raw materials

Raw materials

Preparation Products

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LY-2562175 Suppliers

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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

1103500-20-4

C28H27Cl2N3O4