SRX246是一种强效的、具有中枢神经系统穿透性的血管加压素1a（V1a）受体拮抗剂。
Cas No.:512784-93-9
Sample solution is provided at 25 µL, 10mM.
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SRX246 is a centrally penetrant vasopressin 1a (V1a) receptor antagonist[1-2]. SRX246 has potential applications in treating stress-related disorders and irritability in patients with Huntington's disease[3-4].
In vivo, Beagle dogs were orally administered SRX246 (3, 15, and 75mg/kg) once daily for 28 consecutive days. The oral bioavailability of SRX246 in Beagle dogs was approximately 11%. The plasma exposure (AUC and Cmax) of SRX246 increased with the dose, and no significant toxicity was observed during the 28-day dosing study[5]. In rats, a single oral dose of SRX246 (20mg/kg) was administered. The maximum plasma concentration (Cmax) reached 100ng/ml, with a time to peak (Tmax) of 4 hours and a plasma half-life (T1/2) of 2.5 hours. SRX246 effectively penetrated the blood-brain barrier. The maximum concentration of SRX246 in brain tissue was 20ng/ml, and SRX246 half-life in the brain was approximately 6 hours[6].
References:
[1] Maibach HT, Brownstein MJ, Hersch SM, et al. The Vasopressin 1a Receptor Antagonist SRX246 Reduces Aggressive Behavior in Huntington's Disease. Journal of Personalized Medicine. 2022 Sep;12(10):1561.
[2] Norred MA, Zuschlag ZD, Hamner MB. A Neuroanatomic and Pathophysiologic Framework for Novel Pharmacological Approaches to the Treatment of Post-traumatic Stress Disorder. Drugs. 2024 Feb;84(2):149-164.
[3] Andriessen RL, Oosterloo M, Molema J, et al. Pharmacological Treatment of Neuropsychiatric Symptoms in Huntington's Disease: A Systematic Review. Movement Disorders Clinical Practice. 2025 Apr;12(4):418-431.
[4] Difede J, McAleavey AA, Emrich M, et al. A proof-of-concept randomized crossover clinical trial of a first-in-class vasopressin 1a receptor antagonist for PTSD: Design, methods, and recruitment. Contemporary Clinical Trials Communications. 2023 Jun;33:101116.
[5] Fabio KM, Guillon CD, Lu SF, et al. Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013 Jun;102(6):2033-2043.
[6] Guillon CD, Koppel GA, Brownstein MJ, et al. Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem. 2007 Mar 1;15(5):2054-80.
SRX246是一种强效的、具有中枢神经系统穿透性的血管加压素1a（V1a）受体拮抗剂[1-2]。SRX246可用于治疗与压力有关的疾病和亨廷顿病患者的易激惹性[3-4]。
在体内，口服SRX246（3，15，75mg/kg）处理Beagle Dogs，每日次，连续28天，Beagle Dogs对SRX246的生物利用度约为11%，SRX246的血浆暴露量（AUC和Cmax）随剂量增加而增加，在28天给药研究中未观察到显著的毒性反应[5]。大鼠口服给药SRX246（20mg/kg），SRX246在血浆中的最大浓度为100ng/ml，达峰时间（Tmax）为4小时，血浆半衰期（T1/2）为2.5小时。SRX246能有效穿透血脑屏障。SRX246在脑组织中的最大浓度为20ng/ml，脑内半衰期约为6小时[6]。
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were orally dosed with SRX246 (20mg/kg), formulated in 23% hydroxypropyl beta-cyclodextrin with 0.68% lactic acid. |
Dosage form | 20mg/kg; oral gavage; single dose. |
Applications | SRX246 reached a maximum plasma concentration of 100ng/ml at 4 hours post-administration (Tmax=4 hours). The plasma half-life (T1/2) was 2.5 hours. SRX246 effectively penetrated the blood-brain barrier, achieving a brain Cmax of 20ng/ml. The brain half-life was approximately 6 hours. |
References: | |
| Cas No. | 512784-93-9 | SDF | |
| Canonical SMILES | O=C(N1CCC(N2CCCCC2)CC1)C[C@H](C(N[C@@H](C3=CC=CC=C3)C)=O)N4[C@@H]([C@H](N5[C@@H](C6=CC=CC=C6)COC5=O)C4=O)/C=C/C7=CC=CC=C7 | ||
| 分子式 | C42H49N5O5 | 分子量 | 703.87 |
| 溶解度 | DMSO : 100 mg/mL (142.07 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 | 1.4207 mL | 7.1036 mL | 14.2072 mL |
| 5 mM | 284.1 μL | 1.4207 mL | 2.8414 mL |
| 10 mM | 142.1 μL | 710.4 μL | 1.4207 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。
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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