3089177-97-6
Chemical Structure
RTY-406
- CAS No.: 3089177-97-6
- Formula:C19H17ClN4O3
- Molecular Weight:384.82
InChIKey: SWMITJUPXXOKEK-CYBMUJFWSA-N
SMILES: O=C(N[C@@H]1CCOC2=C1C=NC(C(N)=O)=C2)C(N3C)=CC4=C3C=C(Cl)C=C4
Biological Activity: RTY-406 is an orally active ABCB4/MDR3 and ABCB11/BSEP positive modulator. RTY-406 increases ABCB4/MDR3 and ABCB11/BSEP protein levels and functional output, elevates biliary phospholipid levels, enhances bile acid efflux, increases bile flow and micelle formation, reduces hepatic bile acids, and promotes cholesterol-to-bile-acid conversion. RTY-406 does not induce hepatocellular injury, maintains normal serum alanine transaminase and aspartate aminotransferase levels, and shows a favorable safety profile in cynomolgus monkeys. RTY-406 can be used for the research of primary sclerosing cholangitis and cholestasis[1][2].
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RTY-406 | RTY-406 is an orally active ABCB4/MDR3 and ABCB11/BSEP positive modulator. RTY-406 increases ABCB4/MDR3 and ABCB11/BSEP protein levels and functional output, elevates biliary phospholipid levels, enhances bile acid efflux, increases bile flow and micelle formation, reduces hepatic bile acids, and promotes cholesterol-to-bile-acid conversion. RTY-406 does not induce hepatocellular injury, maintains normal serum alanine transaminase and aspartate aminotransferase levels, and shows a favorable safety profile in cynomolgus monkeys. RTY-406 can be used for the research of primary sclerosing cholangitis and cholestasis. | |||||||||||||||||||||
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References
- [1]. Eric L. Bell, et al. RTY-406, a candidate drug for Primary Sclerosing Cholangitis (PSC), a dual-acting ABCB4/MDR3 and ABCB11/BSEP positive functional modulator, demonstrates proof of mechanism in non-human primates.
- [2]. Eric L. Bell, et al. RTY-406 is a dual-acting ABCB4/MDR3 and ABCB11/BSEP positive functional modulator that demonstrates efficacy in a model of Primary Sclerosing Cholangitis.
