Fedovapagon
(Synonyms: VA106483) 目录号 : GC36037
Fedovapagon 是一种选择性的加压素 V2R 激动剂，EC50 值为 24 nM。被开发用于夜尿症。
Cas No.:347887-36-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia[1]. EC50:24 nM (V2R)[1]
[1]. Yea CM, et al. New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. J Med Chem. 2008 Dec 25;51(24):8124-34.
| Cas No. | 347887-36-9 | SDF | |
| 别名 | VA106483 | ||
| Canonical SMILES | CC1=C(CNC(N2CCC[C@]2(C(N(C)C)=O)[H])=O)C=CC(C(N3CCCCC4=C3C=CC=C4)=O)=C1 | ||
| 分子式 | C27H34N4O3 | 分子量 | 462.58 |
| 溶解度 | DMSO: ≥ 125 mg/mL (270.22 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1618 mL | 10.8089 mL | 21.6179 mL |
| 5 mM | 0.4324 mL | 2.1618 mL | 4.3236 mL |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1618 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。
Lower Urinary Tract Symptoms: What's New in Medical Treatment?
Eur Urol Focus 2018 Jan;4(1):17-24.PMID:29665997DOI:10.1016/j.euf.2018.04.005
Context: Pharmacological treatment is a cornerstone in the management of patients with lower urinary tract symptoms (LUTS). Objective: To review emerging evidence in the medical treatment of LUTS. Evidence acquisition: An Embase/Pubmed-based literature search was conducted in December 2017, screening for randomized controlled trials (RCTs), prospective and retrospective series, animal model studies, and reviews on medical treatment of LUTS. Evidence synthesis: The main medical innovation in recent years in overactive bladder (OAB) has been the approval of the first β3-adrenoceptor agonists (mirabegron) and intradetrusor onabotulinum toxin A, while several other drugs such as antiepileptics, phosphodiesterase inhibitors, or other β3-agonists have brought promising results in phase 3 trials. Intraprostatic injections of various drugs for LUTS/benign prostatic hyperplasia have been investigated, but results of phase 3 trials are still pending, while combination therapies of phosphodiesterase type 5 inhibitors+α-blockers or finasteride have been proved as superior to single therapies in RCTs conducted in these patients. Two new formulations of desmopressin have been approved for nocturia in the USA (desmopressin nasal spray) and Europe/Canada/Australia (desmopressin orally disintegrated tablet). Fedovapagon, a vasopressin V2 receptor agonist, has recently completed a large phase 3 trial in male patients with nocturia. Other phase 3 trials are ongoing in bladder pain syndrome (AQX 11-25, a SHIP-1 activator) and in neurogenic detrusor overactivity (mirabegron and abobotulinum toxin A). Conclusions: Medical treatment of LUTS is a very active research field with recently approved drugs for nocturia (desmopressin acetate nasal spray/orally disintegrated tablet) and numerous emerging drugs currently investigated in OAB, LUTS/benign prostatic hyperplasia, nocturia, bladder pain syndrome, and neurogenic detrusor overactivity. Patient summary: Medical treatment of lower urinary tract symptoms is a very active research field with recently approved drugs for nocturia (desmopressin acetate nasal spray/orally disintegrated tablet) and numerous emerging drugs in overactive bladder, nocturia, neurogenic detrusor overactivity, bladder pain syndrome, or benign prostatic hyperplasia.