LY2562175 free base · Synonyms: LY-2562175 · LY 2562175
LY2562175 is a potent and selective farnesoid X receptor agonist.
For research use only. Not for human or veterinary use.
LY2562175 structure
CAS No.: 1103500-20-4
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 650.00 | BP-02141-100mg | In stock | Get quote |
| 250 mg | USD 1,280.00 | BP-02141-250mg | In stock | Get quote |
| 500 mg | USD 1,980.00 | BP-02141-500mg | In stock | Get quote |
| 1 g | USD 3,200.00 | BP-02141-1g | Inquire | Get quote |
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Description
LY2562175 is a potent and selective farnesoid X receptor (FXR) agonist. LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with EC50 of 193 nM.
Biological activity
In Vitro LY2562175 promotes transcriptional activation of human FXR in a cell-based co-transfection assay with an EC50 of 193 nM. LY2562175 promotes recruitment of a peptide from the nuclear receptor interaction domain of the coactivator SRC-1 with a relative EC50 of 121 nM and 93.5% efficacy as compare to GW4064. 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.
Identifiers
- SMILES
-
CN1C=C(C(O)=O)C2=C1C=C(C=C2)N1CCC(CC1)OCC1=C(ON=C1C1=C(Cl)C=CC=C1Cl)C1CC1 - InChIKey
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RPVDFHPBGBMWID-UHFFFAOYSA-N
Specifications
- MW (average)
- 540.4380
- Formula
- C28H27Cl2N3O4
- CAS No.
- 1103500-20-4
- Physical state
- Solid
- Color
- White to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMF: 20 mg/ml DMSO: 30 mg/ml DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml