SRX246 |
Catalog No.GC38948
One-Click Copy Product Info
|
SRX246은 중추 침투성 혈관가압소 1a (V1a) 수용체 길항제이다.
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.
_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');)
SRX246은 중추 침투성 혈관가압소 1a (V1a) 수용체 길항제이다. SRX246은 스트레스 관련 장애 및 헌팅턴병 환자의 과민성 치료에 잠재적 응용 가능성을 가지고 있다[3-4].
체내 실험에서 비글견에 SRX246 (3, 15, 75mg/kg)을 28일간 매일 1회 경구 투여하였다. 비글견에서 SRX246의 경구 생체이용률은 약 11%였다. SRX246의 혈장 노출량 (AUC 및 Cmax)은 용량 의존적으로 증가하였고 28일 투여 연구 동안 현저한 독성은 관찰되지 않았다[5]. 쥐에서는 SRX246 (20mg/kg)을 단일 경구 투여하였다. 최대 혈장 농도(Cmax)는 100ng/ml에 도달하였고 최고 농도 도달 시간 (Tmax)은 4시간이고 혈장 반감기(T1/2)는 2.5시간이었다. SRX246은 효과적으로 혈관뇌장벽을 침투하였다. 뇌 조직에서 SRX246의 최대 농도는 20ng/ml였고 뇌 내 SRX246 반감기는 약 6시간이었다[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.
| 동물 실험 [1]: | |
동물 모형 | Sprague-Dawley 쥐 |
제조 방법 | 쥐에 SRX246 (20mg/kg)을 23% 히드록시프로필 베타-사이클로덱스트린과 0.68% 젖산으로 배합해서 경구 투여하였습니다. |
제형 | 20mg/kg; 구강 투여; 단일 주사. |
응용 분야 | SRX246은 투여 후 4시간에 최대 혈장 농도 100ng/ml에 도달하였습니다(Tmax=4시간). 혈장 반감기(T1/2)는 2.5시간이었습니다. SRX246은 효과적으로 혈관뇌장벽을 침투해서 뇌 Cmax가 20ng/ml에 달성하였고 뇌 반감기는 약 6시간이었습니다. |
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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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.)