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Size | Price | Stock |
---|---|---|
5mg | $100 | 3-6 Days |
10mg | $150 | 3-6 Days |
25mg | $250 | 3-6 Days |
50mg | $450 | 3-6 Days |
100mg | $700 | 3-6 Days |
250mg | $1100 | 3-6 Days |
500mg | $1450 | 3-6 Days |
Cat #: V2948 CAS #: 900510-03-4 Purity ≥ 98%
Description: Cligosiban (formerly known as PF-3274167) is a novel, potent, selective and high-affinity nonpeptide antagonist of oxytocin receptor (OTR) with Ki of 9.5 nM. 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. PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, nM.
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Molecular Weight (MW) | 419.84 |
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Molecular 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 |
Protocol | 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. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.3819 mL | 11.9093 mL | 23.8186 mL | 47.6372 mL |
5mM | 0.4764 mL | 2.3819 mL | 4.7637 mL | 9.5274 mL |
10mM | 0.2382 mL | 1.1909 mL | 2.3819 mL | 4.7637 mL |
20mM | 0.1191 mL | 0.5955 mL | 1.1909 mL | 2.3819 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.