Balovaptan (RG7314)是一种新型的、具有口服活性的、选择性的、可透过血脑屏障的血管加压素1a受体拮抗剂。
Cas No.:1228088-30-9
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Balovaptan (RG7314) is a novel, orally active, selective, and blood-brain barrier-penetrating vasopressin 1a (V1a) receptor antagonist[1-2]. Balovaptan regulates social behavior by antagonizing the V1a receptor, potentially improving social communication function in individuals with autism spectrum disorder. Balovaptan is applicable for research related to autism spectrum disorder[3-4].
In vivo, mice were pre-treated with an intrathecal injection of Balovaptan (0.1nmol; 5µL). Thirty minutes later, oxytocin (OT; 0.03-3nmol; 50µL) was administered subcutaneously to induce hindpaw scratching behavior. Balovaptan had a significant effect on the OT-induced scratching behavior[5]. Mice that received a single oral dose of Balovaptan (30mg/kg) were subjected to a 6-hour phase advance of their light-dark cycle. Balovaptan significantly shortened the number of days required for the circadian rhythm to resynchronize to the new cycle, thereby accelerating the re-entrainment of the circadian rhythm under simulated jet lag conditions[6].
References:
[1] Zhong P, Chu B, Yu Z, et al. Molecular basis of antagonism of the dimeric human arginine vasopressin receptor 1A. Nature Communications. 2026 Jan;17(1):1622.
[2] Ratni H, Rogers-Evans M, Bissantz C, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.
[3] Dell'Osso L, Bonelli C, Giovannoni F, et al. Available Treatments for Autism Spectrum Disorder: From Old Strategies to New Options. Pharmaceuticals (Basel, Switzerland). 2025 Feb;18(3):324.
[4] Persico AM, Asta L, Chehbani F, et al. The pediatric psychopharmacology of autism spectrum disorder: A systematic review - Part II: The future. Progress in Neuro-psychopharmacology & Biological Psychiatry. 2025 Jan;136:111176.
[5] Guo J, Ba X, Matsuda M, et al. Oxytocin Elicits Itch Scratching Behavior via Spinal GRP/GRPR System. Front Neurosci. 2020 Sep 23;14:581977.
[6] Boareto M, Mendoza J, Holst SC, et al. Modelling the effect of V1a receptor antagonism and its potential therapeutic effect in circadian disorders. bioRxiv; 2025.
Balovaptan (RG7314)是一种新型的、具有口服活性的、选择性的、可透过血脑屏障的血管加压素1a受体拮抗剂[1-2]。Balovaptan通过拮抗V1a受体来调节社交行为，可能改善自闭症患者的社交沟通功能。Balovaptan可用于自闭症谱系障碍的相关研究[3-4]。
在体内，预先鞘内注射Balovaptan（0.1nmol；5μL）小鼠30分钟后，皮下注射催产素（OT；0.03-3nmol；50μL）诱导小鼠后爪搔抓行为。Balovaptan对OT诱导的搔抓行为产生显著影响[5]。单次口服Balovaptan（30mg/kg）处理的小鼠，在经历光照周期6小时相位提前后，Balovaptan显著缩短了节律重新同步到新周期所需的天数，加速了小鼠在时差条件下昼夜节律的重新同步[6]。
| Animal experiment [1]: | |
Animal models | Male and female C57BL/6 mice |
Preparation Method | In studies of oxytocin (OT)-induced itch scratching behavior, a selective vasopressin 1a receptor (V1aR) antagonist, Balovaptan, was used. Mice received intrathecal injection of the V1aR antagonist Balovaptan (0.1nmol, dissolved in 5µL) 15 minutes before the intrathecal administration of OT (0.03nmol). Scratching behaviors were video-recorded and quantified for 30 minutes immediately after OT injection. |
Dosage form | 0.1nmol; i.t.; Pre-treatment (single dose). |
Applications | Pretreatment with the selective V1aR antagonist Balovaptan did not affect OT-induced scratching behaviors. The number of scratching bouts in the Balovaptan + OT group was not significantly different from the vehicle + OT control group. This result suggests that, under the specific conditions of this study (low dose of intrathecal OT), OT-induced scratching behavior is mediated by spinal oxytocin receptors (OTRs) and not by vasopressin 1a receptors (V1aRs). |
References: | |
| Cas No. | 1228088-30-9 | SDF | |
| 别名 | RG7314 | ||
| Canonical SMILES | CN1CC2=NN=C([C@H]3CC[C@H](OC4=NC=CC=C4)CC3)[N@]2[C@]5=CC=C(Cl)C=C5C1 | ||
| 分子式 | C22H24ClN5O | 分子量 | 409.91 |
| 溶解度 | DMSO: 62.5 mg/mL (152.47 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。 |
||
| 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 | 2.4396 mL | 12.1978 mL | 24.3956 mL |
| 5 mM | 487.9 μL | 2.4396 mL | 4.8791 mL |
| 10 mM | 244 μL | 1.2198 mL | 2.4396 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet