WAY-151932 (VNA-932)
(Synonyms: VNA-932; WAY-VNA 932) 目录号 : GC31475
WAY-151932 (VNA-932) 是一种加压素 V2 受体激动剂，在人 V2 结合和 V1a 结合试验中的 IC50 分别为 80.3 nM 和 778 nM。
Cas No.:220460-92-4
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
WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.
WAY-151932 (VNA-932) stimulates cAMP formation in LV2 cells expressing the hV2 receptors in a dose-dependent manner with an EC50 of 0.74±0.07 nM[2].
Oral administration of WAY-151932 (VNA-932) to water-loaded conscious rats produces a dose-dependent decrease in urine volume (ED50=0.14 mg/kg, 2.5% starch in water vehicle) and a corresponding increase in osmolality without altering the urine electrolyte excretion profile[2].
[1]. Molinari AJ, et al. Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5796-800. [2]. Failli AA, et al. Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9.
| Cas No. | 220460-92-4 | SDF | |
| 别名 | VNA-932; WAY-VNA 932 | ||
| Canonical SMILES | O=C(C1=CC=C(N2N=C(C)C=C2)C=C1Cl)N3CC4=CC=CN4CC5=CC=CC=C53 | ||
| 分子式 | C23H19ClN4O | 分子量 | 402.88 |
| 溶解度 | DMSO : 200 mg/mL (496.43 mM; Need ultrasonic) | 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 | 2.4821 mL | 12.4106 mL | 24.8213 mL |
| 5 mM | 0.4964 mL | 2.4821 mL | 4.9643 mL |
| 10 mM | 0.2482 mL | 1.2411 mL | 2.4821 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。
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists
Our efforts in seeking low molecular weight agonists of the antidiuretic peptide hormone arginine vasopressin (AVP) have led to the identification of the clinical candidate WAY-151932 (VNA-932). Further exploration of the structural requirements for agonist activity has provided another class of potent, orally active, non-peptidic vasopressin V2 receptor selective agonists exemplified by the 5,11-dihydro-pyrido[2,3-b][1,5]benzodiazepine as a candidate for further development.
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan
Small molecule agonists and antagonists of the V(2)-vasopressin receptor have been discovered and have undergone clinical trials. In conjunction with these discovery programs, the synthesis and biological testing of various metabolites associated with these clinical targets were actively pursued. We now report the results of our synthetic efforts and the corresponding biological data generated for several of the metabolites of WAY-151932 and CL-347985 (Lixivaptan).