NS 9283 |
Catalog No.GC45987
One-Click Copy Product Info
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NS 9283은 α4β2 아단위 니코틴성 아세틸콜린 수용체(nAChR)의 긍정적인 알로스테릭 변조기이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913830-15-6
Sample solution is provided at 25 µL, 10mM.
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NS 9283은 α4β2 아단위 니코틴성 아세틸콜린 수용체(nAChR)의 긍정적인 알로스테릭 변조기이다. NARCs는 Cys-Loop 수용체 슈퍼가족에서 리간드로 제어되는 카티온을 포함하는 전통적인 막 통로 채널이다. 이러한 수용체의 신경 세포 아형(예: α7과 α4β2 아형)은 불안, 통증, 음식 섭취, 니코틴 추구 행동, 그리고 많은 인지 기능의 중심 처리과 같은 신경행동 과정에 관여한다[2].NS 9283은 주의력 결핍 과잉행동장애(ADHD), 정신분열증, 파킨슨병, 알츠하이머병과 같은 다양한 신경학적 장애를 연구하는데 사용할 수 있다[3, 4]. 전기생리학 실험에서 NS 9283은 (α4)3(β2)2 유형 nAChR의 유도 반응의 진폭을 증가시킬 수 있다[5].
체내 실험에서 NS 9283(3.5mg/kg)은 복강 주사로 투여되고 쥐의 니코틴 자기 투여를 줄였다[6]. NS 9283(3.5μM/kg)은 몇몇 통증/염증성 통증 모델에서 쥐에게 복강 주사되었고 쥐에서 ABT-594의 진통 효과를 강화시켰다[7].
References:
[1] Yakel J L. Functional distribution and regulation of neuronal nicotinic ach receptors in the mammalian brain[J]. Nicotinic Receptors, 2014: 93-114.
[2] Pandya A A, Yakel J L. Effects of neuronal nicotinic acetylcholine receptor allosteric modulators in animal behavior studies[J]. Biochemical pharmacology, 2013, 86(8): 1054-1062.
[3] Hurst R, Rollema H, Bertrand D. Nicotinic acetylcholine receptors: from basic science to therapeutics[J]. Pharmacology & therapeutics, 2013, 137(1): 22-54.
[4] Terry Jr A V, Callahan P M. Nicotinic acetylcholine receptor ligands, cognitive function, and preclinical approaches to drug discovery[J]. Nicotine and Tobacco Research, 2019, 21(3): 383-394.
[5] Timmermann D B, Sandager‐Nielsen K, Dyhring T, et al. Augmentation of cognitive function by NS9283, a stoichiometry‐dependent positive allosteric modulator of α2‐and α4‐containing nicotinic acetylcholine receptors[J]. British journal of pharmacology, 2012, 167(1): 164-182.
[6] Maurer J J, Sandager-Nielsen K, Schmidt H D. Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283[J]. Psychopharmacology, 2017, 234: 475-484.
[7] Zhu C Z, Chin C, Rustay N R, et al. Potentiation of analgesic efficacy but not side effects: co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats[J]. Biochemical pharmacology, 2011, 82(8): 967-976.
| Cas No. | 913830-15-6 | SDF | |
| Canonical SMILES | N#CC1=CC(C2=NC(C3=CN=CC=C3)=NO2)=CC=C1 | ||
| Formula | C14H8N4O | M.Wt | 248.2 |
| Solubility | DMF: 10 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 3 mg/ml,Ethanol: Partially soluble | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.029 mL | 20.145 mL | 40.2901 mL |
| 5 mM | 805.8 μL | 4.029 mL | 8.058 mL |
| 10 mM | 402.9 μL | 2.0145 mL | 4.029 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)