BIO-32546 is an autotaxin (ATX) modulator. BIO-32546 has demonstrated in vivo efficacy in a model of acute pain with good PK/PD correlation. BIO-32546 showed a moderate blocking effect with lowered clearance (CL = 29 mL/min/kg) in rat PK, while maintaining good ATX potency (IC50 = 1.0 ±0.5 nM, N = 5) and low human microsomal clearance (CL =7.6 mL/min/kg). Compound 6 maintained low hERG inhibition (21.3% @ 10 μM) and excellent selectivity over receptors S1P1−5 and LPA1−3,5 (IC50 > 10 μM).
MedKoo Cat#: 462303
Name: BIO-32546
CAS#: 1548743-66-3
Chemical Formula: C28H31F6NO3
Exact Mass: 543.2208
Molecular Weight: 543.55
Elemental Analysis: C, 61.87; H, 5.75; F, 20.97; N, 2.58; O, 8.83
The following data is based on the product molecular weight 543.55 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 |