PRX-08066 free base
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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]).


Price and Availability

Size Price Shipping out time Quantity
100mg USD 1350 2 Weeks
200mg USD 1850 2 Weeks
500mg USD 2150 2 Weeks
1g USD 3250 2 Weeks
2g USD 4250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

PRX-08066, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

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


Technical Data

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


References

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.