SYM 2081
Based on 1 Customer Validation
SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.0%
- CAS No.: 31137-74-3
- 화학식: C6H11NO4
- 분자량:161.16
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Pyroptosis Compound Library
HY-L059
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Neurotransmitter Receptor Compound Library
HY-L062
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Neuroprotective Compound Library
HY-L070
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Mitochondria-Targeted Compound Library
HY-L089
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Anti-Prostate Cancer Compound Library
HY-L124
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
HY-L166
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Multi-Target Compound Library
HY-L176
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Mitophagy Compound Library
HY-L180
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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Kainate Receptor |
Caspase-3 |
Bax |
Bcl-2 |
EAAT1 54 μM (Km) |
EAAT2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4 μM
Compound: SYM-2081
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Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay
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[PMID: 19819046] |
| Oocyte | EC50 |
0.558 μM
Compound: (2S,4R)-4-Me-Glu
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Agonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
Agonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
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[PMID: 21619066] |
| Oocyte | EC50 |
1.55 μM
Compound: (2S,4R)-4-Me-Glu
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Agonist activity at rat GluK2 mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
Agonist activity at rat GluK2 mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
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[PMID: 21619066] |
| Oocyte | EC50 |
45.1 μM
Compound: (2S,4R)-4-Me-Glu
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Agonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
Agonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
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[PMID: 21619066] |
SYM 2081 is transported by EAAT1 expressed in Xenopus laevis oocytes with a Km of 54 μM, while it potently blocks glutamate transport by EAAT2 with a Kb of 3.4 μM[2].
SYM 2081 (10 μg/mL; 16 h) increases Bcl-2 expression and decreases Bax/caspase-3 expression and Bax/Bcl-2 ratio in cultured embryonic cortical neuronal cells under hypoxia[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SYM 2081 (10 mg/kg; i.p.; 30 min before the hypoxic exposure) reduces apoptosis in the hypoxic-ischemic brain of neonatal rats by increasing Bcl-2 expression and decreasing Bax/caspase-3 expression and Bax/Bcl-2 ratio[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (250-300 g); intraplantar capsaicin injection or Carrageenan (HY-125474) injection[3]
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Dosage:10, 50, 100 mg/kg for Capsaicin model; 10, 100 mg/kg (saline) for Carrageenan model
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Administration:i.p. injection once, 30 min before capsaicin or 2.5 h after carrageenan
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Result:Reduced mechanical withdrawal frequency and prolonged heat withdrawal latency at 100 mg/kg (capsaicin model).
Completely reversed mechanical hyperalgesia and partially reversed heat hyperalgesia, with effects lasting 2.5 h and 5.5 h, respectively (Carrageenan model).
Chemical Information
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CAS No. 31137-74-3
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Appearance Solid
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분자량 161.16
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화학식 C6H11NO4
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Color White to off-white
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SMILES
N[C@@H](C[C@@H](C)C(O)=O)C(O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
H2O : 50 mg/mL (310.25 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee JY, et al. Furthering pharmacological and physiological assessment of the glutamatergic receptors at the Drosophila neuromuscular junction. Comp Biochem Physiol C Toxicol Pharmacol. 2009 Nov;150(4):546-57. [Content Brief]
[2]. Vandenberg RJ, et al. Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2. Mol Pharmacol. 1997 May;51(5):809-15. [Content Brief]
[3]. Turner MS, et al. SYM 2081, an agonist that desensitizes kainate receptors, attenuates capsaicin and inflammatory hyperalgesia. Brain Res. 2003 May 30;973(2):252-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 6.2050 mL | 31.0251 mL | 62.0501 mL | 155.1253 mL |
| 5 mM | 1.2410 mL | 6.2050 mL | 12.4100 mL | 31.0251 mL | |
| 10 mM | 0.6205 mL | 3.1025 mL | 6.2050 mL | 15.5125 mL | |
| 15 mM | 0.4137 mL | 2.0683 mL | 4.1367 mL | 10.3417 mL | |
| 20 mM | 0.3103 mL | 1.5513 mL | 3.1025 mL | 7.7563 mL | |
| 25 mM | 0.2482 mL | 1.2410 mL | 2.4820 mL | 6.2050 mL | |
| 30 mM | 0.2068 mL | 1.0342 mL | 2.0683 mL | 5.1708 mL | |
| 40 mM | 0.1551 mL | 0.7756 mL | 1.5513 mL | 3.8781 mL | |
| 50 mM | 0.1241 mL | 0.6205 mL | 1.2410 mL | 3.1025 mL | |
| 60 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5854 mL | |
| 80 mM | 0.0776 mL | 0.3878 mL | 0.7756 mL | 1.9391 mL | |
| 100 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5513 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SYM 2081 Related Classifications
HY-101310 Related Classifications
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