1428988-21-9
Chemical Structure
BAY-1128688
- CAS No.: 1428988-21-9
- Formula:C28H31FN2O3
- Molecular Weight:462.56
InChIKey: JFRWOHRGXFCADF-XVTSZCMISA-N
SMILES: C[C@@]12[C@](CC=C2C3=CN=CC(F)=C3)([H])[C@@]4([H])[C@@](CC1)([H])C5=CC=C(C(N(C)CCC(O)=O)=O)C=C5CC4
Biological Activity: BAY-1128688 is a selective, orally active aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 of 1.4 nM. BAY-1128688 inhibits OATP, BSEP, MRP4, NTCP, UGT1A1, MRP2, and MRP3. BAY-1128688 induces reactive oxygen species (ROS) production, inhibits the mitochondrial electron transport chain, and increases circulating androsterone, etiocholanolone, dihydrotestosterone, and serum bilirubin concentrations. BAY-1128688 alters bilirubin disposition, leading to elevated plasma bilirubin, independent of liver injury. BAY-1128688 can be used in research on endometriosis and polycystic ovary syndrome[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BAY-1128688 | 98.49% | BAY-1128688 is a selective, orally active aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 of 1.4 nM. BAY-1128688 inhibits OATP, BSEP, MRP4, NTCP, UGT1A1, MRP2, and MRP3. BAY-1128688 induces reactive oxygen species (ROS) production, inhibits the mitochondrial electron transport chain, and increases circulating androsterone, etiocholanolone, dihydrotestosterone, and serum bilirubin concentrations. BAY-1128688 alters bilirubin disposition, leading to elevated plasma bilirubin, independent of liver injury. BAY-1128688 can be used in research on endometriosis and polycystic ovary syndrome. | ||||||||||||||||||||
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References
- [1]. Battista C, et al. Quantitative Systems Toxicology Identifies Independent Mechanisms for Hepatotoxicity and Bilirubin Elevations Due to AKR1C3 Inhibitor BAY1128688. Clinical pharmacology and therapeutics. 2023 Nov;114(5):1023-1032.
- [2]. Gashaw I, et al. Novel aldo-keto reductase 1C3 inhibitor affects androgen metabolism but not ovarian function in healthy women: a phase 1 study. European journal of endocrinology. 2023 Jul 10;188(7):578-591.
- [3]. Cascorbi I. Clinical Pharmacology of Cannabinoid Therapeutics: Drug Interactions and Side Effects. Clin Pharmacol Ther. 2023 Nov;114(5):943-946.
