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 maleate

PRX-08066 maleate maleate 是一种具有口服活性和选择性的 5-羟色胺受体 2B (5-HT2BR) 拮抗剂，其 Ki 为 3.4 nM。PRX-08066 maleate maleate 可抑制 MAPK 通路、5-HT 释放以及纤维化因子 (TGFβ1、CTGF 和 FGF2) 的表达。PRX-08066 maleate maleate 可抑制 KRJ-I 细胞增殖并诱导细胞凋亡 (apoptosis) (激活 caspase-3)。PRX-08066 maleate maleate 可抑制肺血管重塑。PRX-08066 maleate maleate 可用于治疗肺动脉高压 (PAH) 和神经内分泌肿瘤 (NET)。

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PRX-08066 maleate

PRX-08066 maleate Chemical Structure

CAS No. : 866206-55-5

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PRX-08066 maleate 的其他形式现货产品:

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PRX-08066 maleate 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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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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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

  • 生物活性

  • 纯度 & 产品资料

生物活性

PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET)[1][2].

IC50 & Target[1]

5-HT2B Receptor

3.4 nM (Ki)

体外研究
(In Vitro)

PRX-08066 maleate 抑制 5-HT 诱导的丝裂原活化蛋白激酶活化 (IC50 = 12 nM)，并显著降低表达人类 5-HT2BR 的仓鼠卵巢细胞中的胸苷掺入 (IC50 = 3 nM)[1]。
PRX-08066 (0.01 pM-100 pM，24 小时) maleate 显著抑制 KRJ-I 细胞增殖，IC50 为 4.6 pM，而对 NCI-H720 细胞 (无 5-HT2B 受体表达) 无显著影响[2]。
PRX-08066 (0.01 pM-100 pM) maleate 抑制基础和 Isoproterenol (HY-B0468) 刺激的 5-HT 分泌，在 KRJ-I 细胞中的 IC50 分别为 6.9 pM 和 1.25 pM[2]。
PRX-08066 (0.5 pM) maleate 显著降低 KRJ-I 细胞中 ERK 的磷酸化水平[2]。
PRX-08066 (1-2 小时) maleate 可降低 KRJ-I 细胞中的纤维化因子 (TGFβ1、CTGF、FGF2)[2]。
PRX-08066 (1 pM，24 小时) maleate 通过激活共培养系统中建立的 KRJ-I 细胞和 HEK293 细胞中的 Caspase-3 显著增加凋亡细胞的比例[2]。

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

PRX-08066 maleate 相关抗体:

Cell Viability Assay[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.
体内研究
(In Vivo)

PRX-08066 (50-100 mg/kg，口服，每日两次，持续 5 周) maleate 可改善 Monocrotaline (MCT) (HY-N0750) 诱发的肺动脉高压 (PAH) 大鼠的肺血管重塑、右心室肥大和心脏功能[1]。

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
分子量

517.96

Formula

C23H21ClFN5O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料

PRX-08066 maleate 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-08066866206-55-5PRX08066PRX 080665-HT Receptorp38 MAPKTGF-β ReceptorFGFRApoptosisCaspaseSerotonin Receptor5-hydroxytryptamine ReceptorTransforming growth factor beta receptorsFibroblast growth factor receptorcarcinoidcoculturefibrosisgastrointestinalHEK293KRJ-Ineuroendocrine tumorproliferationserotonintumor microenvironmentInhibitorinhibitorinhibit

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