| Identification | Back Directory | [Name]
KDM5A-IN-1 | [CAS]
1905481-36-8 | [Synonyms]
KDM5A-IN-1
KDM5A inhibitor 1
KDM5A IN 1,KDM5AIN1,KDM-5A-IN-1
Cyclopropanecarboxamide, N-[(3R)-1-[[5-(1-methylethyl)-1H-pyrazol-3-yl]carbonyl]-3-pyrrolidinyl]- | [Molecular Formula]
C15H22N4O2 | [MDL Number]
MFCD29924745 | [MOL File]
1905481-36-8.mol | [Molecular Weight]
290.36 |
| Chemical Properties | Back Directory | [Boiling point ]
592.6±50.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 50 mg/mL (172.20 mM) | [form ]
Solid | [pka]
12.68±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B)[1]. | [in vivo]
KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t1/2 of 0.4 hours[1]. | Animal Model: | Female CD-1 mice[1] | | Dosage: | 5 mg/kg | | Administration: | Oral administration (Pharmacokinetic study) | | Result: | Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%).
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| [IC 50]
KDM5 | [storage]
Store at -20°C | [References]
[1] Liang J, et al. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. DOI:10.1016/j.bmcl.2017.05.016 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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