2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. SYM 2081

SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.

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SYM 2081 Chemical Structure

SYM 2081 Chemical Structure

CAS No. : 31137-74-3

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Based on 1 publication(s) in Google Scholar

SYM 2081 Related Antibodies

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AMPA Receptor NMDA Receptor Kainate Receptor

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Description

SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively[1].

IC50 & Target

Kainate Receptor

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
4 μM
Compound: SYM-2081
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
[PMID: 19819046]
Oocyte EC50
0.558 μM
Compound: (2S,4R)-4-Me-Glu
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
[PMID: 21619066]
Oocyte EC50
1.55 μM
Compound: (2S,4R)-4-Me-Glu
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
[PMID: 21619066]
Oocyte EC50
45.1 μM
Compound: (2S,4R)-4-Me-Glu
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
[PMID: 21619066]
Molecular Weight

161.16

Formula

C6H11NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](C[C@@H](C)C(O)=O)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (310.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.2050 mL 31.0251 mL 62.0501 mL
5 mM 1.2410 mL 6.2050 mL 12.4100 mL
View the 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.

* 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

SDS (251 KB)

COA (246 KB) HNMR (244 KB) MS (177 KB)

Handling Instructions (2659 KB)
References

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.

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SYM 2081 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SYM 208131137-74-3SYM2081SYM-2081iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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