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 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 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 可抑制 KRJ-I 细胞增殖并诱导细胞凋亡 (apoptosis) (激活 caspase-3)。PRX-08066 可抑制肺血管重塑。PRX-08066 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

PRX-08066 Chemical Structure

CAS No. : 866206-54-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1326
In-stock
1 mg ￥694
In-stock
5 mg ￥1500
In-stock
10 mg ￥2200
In-stock
25 mg ￥4500
In-stock
50 mg 现货 询价
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500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of PRX-08066:

PRX-08066 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

查看 Caspase 亚型特异性产品:

查看所有亚型
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

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(In Vitro)

PRX-08066 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) 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) 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) 显著降低 KRJ-I 细胞中 ERK 的磷酸化水平[2]。
PRX-08066 (1-2 小时) 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) 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 相关抗体:

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.
体内研究
(In Vivo)

PRX-08066 (50-100 mg/kg，口服，每日两次，持续 5 周) 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

401.89

Formula

C19H17ClFN5S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 7 mg/mL (17.42 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PRX-08066 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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目录号：
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