CAS NO: | 900510-03-4 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 419.84 |
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Formula | C19H19ClFN5O3 |
CAS No. | 900510-03-4 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 10 mM in DMSO |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Solubility (In vivo) | COC1=NC=C(N2C(N3CC(OC4=CC=C(F)C=C4Cl)C3)=NN=C2COC)C=C1 |
Synonyms | cligosiban; PF-03274167; PF 03274167; PF03274167; PF-3274167; PF 3274167; PF3274167 |
In Vitro | In vitro activity: PF-3274167 is a selective and high-affinity nonpeptide antagonist of oxytocin receptor (OTR) with Ki of 9.5nM. PF-3274167 displayed promising in vivo pharmacokinetics and significantly improved aqueous solubility over related compounds containing a biaryl substituent. Oxytocin receptor is a G protein-coupled receptor/protein which functions as receptor for the hormone and neurotransmitter oxytocin. Oxytocin receptors are also present in the central nervous system. Kinase Assay: PF-3274167 is a selective and high-affinity nonpeptide antagonist of oxytocin receptor (OTR) with Ki of 9.5nM. Cell Assay: |
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In Vivo | PF-3274167 displayed promising in vivo pharmacokinetics and significantly improved aqueous solubility over related compounds containing a biaryl substituent. Oxytocin receptor is a G protein-coupled receptor/protein which functions as receptor for the hormone and neurotransmitter oxytocin. Oxytocin receptors are also present in the central nervous system. |
Animal model | |
Formulation & Dosage | |
References | Bioorg Med Chem Lett. 2010 Jan 15;20(2):516-20; J Med Chem. 2015 Mar 12;58(5):2547-52. |