SYM 2081

Name: SYM 2081
Brand: MedChemExpress
SKU: HY-101310
Rating: 4.5 (1 reviews)

Cat. No.: HY-101310 Purity: ≥98.0%: Data Sheet
SDS

COA
Handling Instructions
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SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (K_m of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (K_b 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.

For research use only. We do not sell to patients.

SYM 2081 Chemical Structure

CAS No. : 31137-74-3

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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AMPA Receptor NMDA Receptor Kainate Receptor

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EAAT1 EAAT2 EAAT3 EAAT4 EAAT5

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]^[3]^[4]

Kainate Receptor

Caspase-3

Bax

Bcl-2

EAAT1

54 μM (Km)

EAAT2

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]

In Vitro

SYM 2081 is transported by EAAT1 expressed in Xenopus laevis oocytes with a K_m of 54 μM, while it potently blocks glutamate transport by EAAT2 with a K_b 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.

In Vivo

SYM 2081 (10-100 mg/kg; i.p.; before Capsaicin) attenuates Capsaicin (HY-10448)-evoked mechanical and heat hyperalgesia in rats^[3].
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.

Animal Model:	Adult male Sprague-Dawley rats (250-300 g); intraplantar capsaicin injection or Carrageenan (HY-125474) injection^[3]
Dosage:	10, 50, 100 mg/kg for Capsaicin model; 10, 100 mg/kg (saline) for Carrageenan model
Administration:	i.p. injection once, 30 min before capsaicin or 2.5 h after carrageenan
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).

Molecular Weight

161.16

Formula

C₆H₁₁NO₄

CAS No.

31137-74-3

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
10 mM	0.6205 mL	3.1025 mL	6.2050 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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%

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Data Sheet (287 KB) SDS (251 KB)

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

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]

[4]. Park J K, et al. SYM 2081 Exerts Neuroprotective Effect Modulating Anti-Apoptosis in the Hypoxic-Ischemic Brain Injury of Neonatal Rats[J]. Perinatology, 2019, 30(3): 117-125.

Complete Stock Solution Preparation Table

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

Neurological Disease Inflammation/Immunology Cardiovascular Disease

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-2081iGluREAATBcl-2 FamilyCaspaseIonotropic glutamate receptorsExcitatory amino acid transporter Glutamate transporter;Inhibitorinhibitorinhibit

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SYM 2081

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SYM 2081 Related Antibodies

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SYM 2081 Related Antibodies

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Complete Stock Solution Preparation Table

SYM 2081 Related Classifications

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