Chemical Property of 4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine
Chemical Property:
- Vapor Pressure:4.13E-09mmHg at 25°C
- Boiling Point:472.8°C at 760 mmHg
- Flash Point:239.8°C
- PSA：51.80000
- Density:1.213
- LogP:5.52470
- Storage Temp.:Desiccate at +4°C
- Solubility.:≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
- XLogP3:4
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:2
- Exact Mass:281.13282569
- Heavy Atom Count:21
- Complexity:349
- Purity/Quality:
-
97% *data from raw suppliers
RS 127445 hydrochloride *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N
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Description
RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM). It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT . It also blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner. Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.
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Uses
RS-127445 is a 5-HT2B receptor antagonist with modest activity against other 5-HT receptors. Selective 5-HT2B receptor antagonist
