BI-2081 is a partial agonist on GPR40 with a good in vitro potency (EC50 = 4 nM). The activation of GPR40 allows a glucose depending insulin secretion and BI-2081 significantly reduces the plasma glucose concentration in Zucker diabetic fatty (ZDF) rats. This mode of action allows a high anti-hyperglycemic efficacy with low risk for hypoglycemia. BI-2081 possesses a good in vitro and in vivo PK profile, which makes an oral application with high bioavailability possible. The structurally related BI-0340 is a suitable negative control due to its significant lower potency on GPR40.
MedKoo Cat#: 464521
Name: BI-2081
CAS#: unknown
Chemical Formula: C32H35FO6
Exact Mass: 534.2418
Molecular Weight: 534.62
Elemental Analysis: C, 71.89; H, 6.60; F, 3.55; O, 17.96
The following data is based on the product molecular weight 534.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
