WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 526697
CAS#: 866206-54-4
Description: PRX-08066 is a a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. In the 5-HT(2B) expressing SI-NET cell line, KRJ-I, PRX-08066 inhibited proliferation (IC(50) 4.6 x 10(-9)M) and 5-HT secretion (6.9 x 10(-9)M) and decreased ERK1/2 phosphorylation and profibrotic growth factor synthesis and secretion (transforming growth factor beta 1 [TGFbeta1], connective tissue growth factor [CTGF] and fibroblast growth factor [FGF2]).
MedKoo Cat#: 526697
Name: PRX-08066 free base
CAS#: 866206-54-4
Chemical Formula: C19H17ClFN5S
Exact Mass: 401.0877
Molecular Weight: 401.8884
Elemental Analysis: C, 56.78; H, 4.26; Cl, 8.82; F, 4.73; N, 17.43; S, 7.98
Related CAS #: 866206-55-5(PRX-08066 Maleate)
Synonym: PRX-08066; PRX 08066; PRX08066.
IUPAC/Chemical Name: 5-((4-(6-Chlorothieno(2,3-d)pyrimidine-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile
InChi Key: RPYIKXHIQXRXEM-BTJKTKAUSA-N
InChi Code: InChI=1S/C19H17ClFN5S.C4H4O4/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;5-3(6)1-2-4(7)8/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25);1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code: N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 401.8884 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Kim SK, Li Y, Abrol R, Heo J, Goddard WA 3rd. Predicted structures and
dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C
receptors. J Chem Inf Model. 2011 Feb 28;51(2):420-33. doi: 10.1021/ci100375b.
Epub 2011 Feb 7. PubMed PMID: 21299232; PubMed Central PMCID: PMC3070210.
2: Svejda B, Kidd M, Giovinazzo F, Eltawil K, Gustafsson BI, Pfragner R, Modlin
IM. The 5-HT(2B) receptor plays a key regulatory role in both neuroendocrine
tumor cell proliferation and the modulation of the fibroblast component of the
neoplastic microenvironment. Cancer. 2010 Jun 15;116(12):2902-12. doi:
10.1002/cncr.25049. PubMed PMID: 20564397.
3: Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ,
Shacham S, Al-Mousily F. 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. 2010
Aug;334(2):364-72. doi: 10.1124/jpet.109.165001. Epub 2010 Apr 29. PubMed PMID:
20430844.
4: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin
Pharmacol. 2008 Sep;30(7):543-88. PubMed PMID: 18985183.
