PRX-08066 Maleic acid
目录号 : GC16788
5-HT2B receptor antagonist,potent and selective
Cas No.:866206-55-5
Sample solution is provided at 25 µL, 10mM.
PRX-08066 Maleic acid is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist [1].
5-HT receptors are a group of G protein-coupled receptors and play an important role in schizophrenia, feeding disorders, perception, depression, migraines, hypertension, anxiety, hallucinogens, and gastrointestinal dysfunctions.
In NET cell line, KRJ-I, PRX-08066 inhibited 5-HT secretion and cell proliferation and decreased ERK1/2 phosphorylation and profibrotic growth factor synthesis and secretion (TGFβ1, CTGF and FGF2). In the KRJ-I:HEK293 coculture system, PRX-08066 significantly reduced 5-HT release, Ki67, CTGF, TGFβ1 and FGF2 transcription in the KRJ-I cell line. 5-HT itself stimulated HEK293 proliferation [2].
PRX-08066 has preclinical safety profile, good bioavailability, and low acute toxicity, which is under phase II clinical trials for the treatment of hypoxia-induced pulmonary hypertension syndromes and pulmonary hypertension [3].
In the monocrotaline (MCT)-induced PAH male rats model, PRX-08066 (100 mg/kg) significantly increased right ventricular ejection fraction and reduced peak PA pressure at 50 and 100 mg/kg. Morphometric assessment of pulmonary arterioles showed PRX-08066 significantly reduced medial wall thickening, lumen occlusion and RV hypertrophy. Also, PRX-08066 diminished pulmonary vascular remodeling [1].
References:
[1]. Porvasnik SL, Germain S, Embury J, 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, 334(2): 364-372.
[2]. Svejda B, Kidd M, Giovinazzo F, 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. Cance, 2010, 116(12): 2902-2912.
[3]. Kim SK, Li Y, Abrol R, et al. Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors. J Chem Inf Model, 2011, 51(2): 420-433.
Cas No. | 866206-55-5 | SDF | |
Canonical SMILES | FC(C=C1)=C(C#N)C=C1CN(CC2)CCC2NC3=C(C=C(Cl)S4)C4=NC=N3.O=C(O)/C=C\C(O)=O | ||
分子式 | C19H17ClFN5S.C4H4O4 | 分子量 | 517.96 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
![]() |
1 mg | 5 mg | 10 mg |
1 mM | 1.9307 mL | 9.6533 mL | 19.3065 mL |
5 mM | 0.3861 mL | 1.9307 mL | 3.8613 mL |
10 mM | 0.1931 mL | 0.9653 mL | 1.9307 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet