Referencia número: HY-15472

PRX-08066

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PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).

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Pureza: 97.46%
No. CAS: 866206-54-4
Fòrmula: C₁₉H₁₇ClFN₅S
Peso molecular:401.89

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PRX-08066 Chemical Structure

No. CAS: 866206-54-4

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

5-HT_2B Receptor

3.4 nM (IC₅₀)

Ver todos los productos específicos de isoformas 5-HT Receptor :

Ver todos los productos específicos de isoformas p38 MAPK :

Ver todos los productos específicos de isoformas TGF-β Receptor :

Ver todos los productos específicos de isoformas Caspase :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	270 nM Compound: A	Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin	[PMID: 19307114]
CHO-K1	IC₅₀	3.5 nM Compound: A	Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay	[PMID: 19307114]

In Vitro

PRX-08066 inhibits 5-HT induced mitogen-activated protein kinase activation (IC₅₀ = 12 nM) and markedly reduced thymidine incorporation (IC₅₀ = 3 nM) in hamster ovary cells expressing the human 5-HT2BR^[1].
. PRX-08066 (0.01 pM-100 pM, 24 h) significantly inhibits the proliferation of KRJ-I cells with an IC₅₀ of 4.6 pM and has no significant effect on NCI-H720 cells (with no expression of 5-HT2B receptors)^[2].
PRX-08066 (0.01 pM-100 pM) inhibits basal and Isoproterenol (HY-B0468)-stimulated 5-HT secretion with IC₅₀s of 6.9 pM and 1.25 pM in KRJ-I cells^[2].
PRX-08066 (0.5 pM) significantly reduces the phosphorylation level of ERK in KRJ-I cells^[2].
PRX-08066 (1-2 h) reduces fibrotic factors (TGFβ1, CTGF, FGF2) in KRJ-I cells^[2].
PRX-08066 (1 pM, 24 h) significantly increases the proportion of apoptotic cells by activating Caspase-3 in KRJ-I cells and HEK293 cells established in a coculture system^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[2]

Cell Line:

KRJ-I cells and HEK293 cells established in a coculture system
Concentration:

1 pM
Incubation Time:

24 h
Result:

Significantly increased the proportion of dead cells in KRJ-I, and the proportion of Caspase-3 positive cells among the dead cells also rose.
Significantly increased the proportion of positive cells for Caspase-3 in HEK293 cells.

In Vivo

PRX-08066 (50-100 mg/kg, p.o., twice daily for 5 weeks) improves pulmonary vascular remodeling, right ventricular hypertrophy and cardiac function in Monocrotaline (MCT) (HY-N0750)-induced PAH rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

MCT induced PAH model established in male Sprague-Dawley rats (200-225 g)^[1]
Dosage:

50 and 100 mg/kg
Administration:

Oral administration (p.o.), once daily for 5 weeks
Result:

Selectively reduced pulmonary artery pressure without affecting systemic blood pressure.
Reversed right ventricular hypertrophy.
Reduced the thickness of the media layer of pulmonary small arteries, improves the closure of the lumen, and reduces tissue pathological damage.
Inhibited the proliferation and contraction of vascular smooth muscle mediated by 5-HT.
No significant gastrointestinal side effects or systemic toxicity.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 866206-54-4
Appearance Solid
Peso molecular 401.89
Fòrmula C₁₉H₁₇ClFN₅S
Color White to off-white
SMILES

N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 7 mg/mL (17.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4882 mL

12.4412 mL

24.8824 mL

5 mM

0.4976 mL

2.4882 mL

4.9765 mL

10 mM

0.2488 mL

1.2441 mL

2.4882 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Porvasnik SL, 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. 2010 Aug;334(2):364-72. [Content Brief]

[2]. Svejda B, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4882 mL	12.4412 mL	24.8824 mL	62.2061 mL
	5 mM	0.4976 mL	2.4882 mL	4.9765 mL	12.4412 mL
	10 mM	0.2488 mL	1.2441 mL	2.4882 mL	6.2206 mL
	15 mM	0.1659 mL	0.8294 mL	1.6588 mL	4.1471 mL

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PRX-08066

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Ver todos los productos específicos de isoformas 5-HT Receptor

Ver todos los productos específicos de isoformas p38 MAPK

Ver todos los productos específicos de isoformas TGF-β Receptor

Ver todos los productos específicos de isoformas Caspase

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PRX-08066 Related Classifications

HY-15472 Related Classifications