4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]-
- CAS No.
- 2360853-16-1
- Chemical Name:
- 4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]-
- Synonyms
- RBN-3143, 10 mM in DMSO;4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]-
- CBNumber:
- CB69278815
- Molecular Formula:
- C22H28FN3O4S
- Molecular Weight:
- 449.54
- MDL Number:
- MOL File:
- 2360853-16-1.mol
4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]- Chemical Properties,Uses,Production
Uses
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation[1].
in vivo
RBN-3143 (5 μg; intranasal administration) can improve steroid-resistant asthma mouse models[1].
Animal Model: | Mouse of asthma models[1] |
Dosage: | 5 ug |
Administration: | Intranasal administration |
Result: | Suppressed the accumulation of alarmins TSLP, IL-33, and IL-25. |
IC 50
PARP14: 4 nM (IC50); PARP10: 1600 nM (IC50); PARP15: 4200 nM (IC50); PARP4: 42700 nM (IC50); PARP3: >100000 nM (IC50); PARP2: >100000 nM (IC50); PARP1: >100000 nM (IC50)
References
[1] Niepel M, et, al. The PARP14 inhibitor RBN-3143 suppresses lung inflammation in preclinical models. European Respiratory Journal?2022?60:?4642.
4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
4(3H)-Quinazolinone, 7-[(1-acetyl-4-piperidinyl)methoxy]-5-fluoro-2-[[(tetrahydro-2H-pyran-4-yl)thio]methyl]- Suppliers
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