| Identification | Back Directory | [Name]
KPR-2579 | [CAS]
1801742-41-5 | [Synonyms]
KPR-2579
Benzeneacetamide, α-[benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-, (αR)- | [Molecular Formula]
C23H20F2N2O2 | [MOL File]
1801742-41-5.mol | [Molecular Weight]
394.41 |
| Chemical Properties | Back Directory | [Boiling point ]
577.5±50.0 °C(Predicted) | [density ]
1.272±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
15.05±0.50(Predicted) | [color ]
white to beige | [Optical Rotation]
[α]/D +124 to +136°, c =c=1 in chloroform-d |
| Hazard Information | Back Directory | [Biological Activity]
KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs)stimulated by acetic acid (AA).''KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca2+ response in human/r at CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca2+ influx using hTRPA1hTRPV1or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects. |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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