2. GPCR/G Protein Neuronal Signaling MAPK/ERK Pathway TGF-beta/Smad Protein Tyrosine Kinase/RTK Apoptosis
  3. 5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase
  4. PRX-08066

PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki 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).

For research use only. We do not sell to patients.

PRX-08066

PRX-08066 Chemical Structure

CAS No. : 866206-54-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of PRX-08066:

PRX-08066 Related Antibodies

Top Publications Citing Use of Products

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki 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)[1][2].

IC50 & Target

5-HT2B Receptor

3.4 nM (IC50)

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.

PRX-08066 Related Antibodies

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.
Clinical Trial
Molecular Weight

401.89

Formula

C19H17ClFN5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4882 mL 12.4412 mL 24.8824 mL
5 mM 0.4976 mL 2.4882 mL 4.9765 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRX-08066866206-54-4PRX08066PRX 080665-HT Receptorp38 MAPKTGF-β ReceptorFGFRApoptosisCaspaseSerotonin Receptor5-hydroxytryptamine ReceptorTransforming growth factor beta receptorsFibroblast growth factor receptorcarcinoidcoculturefibrosisgastrointestinalHEK293KRJ-Ineuroendocrine tumorproliferationserotonintumor microenvironmentInhibitorinhibitorinhibit

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