SRX246 |
Catalog No.GC38948
One-Click Copy Product Info
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SRX246 is a centrally penetrant vasopressin 1a (V1a) receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | ||
| Formula | C42H49N5O5 | M.Wt | 703.87 |
| Solubility | DMSO : 100 mg/mL (142.07 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)