A 5-HT2B receptor antagonist
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PRX-08066

Item No. 31477

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-benzonitrile
CAS Number
866206-54-4
Molecular Formula
C19H17ClFN5S
Formula Weight
401.9
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 96mg/mlEthanol: 91 mg/mlWater: 95 mg/ml
λmax
221, 279 nm
SMILES
ClC1=CC(C(S1)=NC=N2)=C2NC3CCN(CC3)CC4=CC(C#N)=C(C=C4)F
InChi Code
InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25)
InChi Key
IENZFHBNCRQMNP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $81

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    Product Description

    PRX-08066 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.1 It binds to 5-HT2B receptors (Ki = 3.4 nM) and inhibits 5-HT-induced MAPK activation and thymidine incorporation in CHO cells expressing human 5-HT2B (IC50s = ~12 and ~3 nM, respectively). PRX-08066 (50 and 100 mg/kg) reduces peak pulmonary arterial pressure and right ventricular hypertrophy in a rat model of pulmonary hypertension induced by monocrotaline (MCT; Item No. 16666).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Porvasnik, S.L., Germain, S., Embury, J., et al. PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. J. Pharmacol. Exp. Ther. 334(2), 364-372 (2010).