PRX-08066 free base | CAS#866206-54-4 | 5-hydroxytryptamine receptor 2B antagonist

PRX-08066 free base
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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 (PAH) and right ventricular hypertrophy in rats.

Chemical Structure

PRX-08066 free base

CAS# 866206-54-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526697
Name: PRX-08066 free base
CAS#: 866206-54-4
Chemical Formula: C19H17ClFN5S
Exact Mass: 401.09
Molecular Weight: 401.890
Elemental Analysis: C, 56.78; H, 4.26; Cl, 8.82; F, 4.73; N, 17.43; S, 7.98

Price and Availability

Size	Price	Availability
100mg	USD 950	2 Weeks
200mg	USD 1650	2 Weeks
500mg	USD 3650	2 Weeks
1g	USD 5450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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, ethanol, and 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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	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]).
In vitro activity:	PRX-08066 demonstrated promising effects in the context of small intestinal neuroendocrine tumors (SI-NETs). and PRX-08066 showed the ability to inhibit both tumor cell proliferation and the secretion of 5-HT. In the cell line KRJ-I, PRX-08066 inhibited cell growth and 5-HT release and reduced the activation of signaling pathways involved in fibrosis and the synthesis of fibrotic growth factors such as TGFbeta1, CTGF, and FGF2. Reference: Cancer. 2010 Jun 15;116(12):2902-12. https://pubmed.ncbi.nlm.nih.gov/20564397/
In vivo activity:	In a PAH rat model, PAH rats were administered PRX-08066 orally for five weeks. The results revealed significant improvements in right ventricular ejection fraction, reduced peak pulmonary artery pressure, reduced pulmonary arteriole wall thickening and lumen occlusion, and decreased right ventricle size compared to the MCT control group. Reference: J Pharmacol Exp Ther. 2010 Aug;334(2):364-72. https://pubmed.ncbi.nlm.nih.gov/20430844/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	96.0	238.87
	Ethanol	91.0	226.43
	Water	95.0	236.38

Preparing Stock Solutions

The following data is based on the product molecular weight 401.89 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

Formulation protocol:	1. 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. PMID: 20564397. 2. 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. PMID: 20430844.
In vitro protocol:	1. 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. PMID: 20564397.
In vivo protocol:	1. 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. PMID: 20430844.

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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.

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