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  4. (RS)-(Tetrazol-5-yl)glycine

(RS)-(Tetrazol-5-yl)glycine  (Synonyms: D,L-(tetrazol-5-yl)glycine; LY 285265)

Cat. No.: HY-100839 Purity: 96.53%
Handling Instructions Technical Support

(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice.

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(RS)-(Tetrazol-5-yl)glycine Chemical Structure

(RS)-(Tetrazol-5-yl)glycine Chemical Structure

CAS No. : 138199-51-6

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Description

(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist[1]. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively[2]. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice[3].

IC50 & Target

NMDA Receptor

 

In Vitro

(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a agonist of N-methyl-D-aspartate (NMDA) subtype of excitatory amino acid receptor. (RS)-(Tetrazol-5-yl)glycine displaces NMDA receptor binding to rat brain membranes as measured using [3H]CGS19755 (IC50=98 nM) and [3H]glutamate (IC50=36 nM) as ligands[1].
(RS)-(Tetrazol-5-yl)glycine does not appreciably inhibit the binding of D,L-alpha-[5-methyl-3H] amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), [3H]kainate, or [3H]glycine (IC50s>30 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(RS)-(Tetrazol-5-yl)glycine can be used in animal modeling to create epilepsy models and is able to penetrate the blood-brain barrier[4].

1. Induction of epilepsy[4]
Background
(RS)-(Tetrazol-5-yl)glycine can stimulate NMDA receptors, causing hippocampal neurotoxic damage and leading to epilepsy.
Specific Modeling Methods
Rat: Sprague-Dawley • male or female • 2-6 months old
Administration: 0.2 and 0.4 μL of a 0.7 mM (RS)-(Tetrazol-5-yl)glycine solution • ICV
Note
(1) Inject (RS)-(Tetrazol-5-yl) glycine into the right ventricle of rats, and after 10 minutes, remove the needle and suture the wound and scalp.
(2) Among the 11 rats injected with 0.28 nmol (RS)-(Tetrazol-5-yl) glycine, 5 died within a few hours after injection, making it impossible to perfuse and determine the degree of hippocampal lesions.
(3) There was no loss of hippocampal neurons in two of the four rats injected with the lower dose of (RS) - (Tetrazol-5-yl) glycine, whereas the other two showed loss of pyramidal neurons in the medial portion of CA1, and granule neurons in the dentate gyrus.
Modeling Indicators
Phenotypic observation: All rats injected with the higher dose of TZG showed an extensive loss of pyramidal neurons and GluR1 immunoreactivity in CA1-4 and in the dentate gyrus.
Behavioral observation: Continuous flicking of the tail, rowing movements, and convulsions.
Correlated Product(s): /
Opposite Product(s): Suramin (HY-B0879)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[3]
Dosage: 1.25, 1.5 mg/kg
Administration: IP
Result: Induced seizure responses and Fos.
Molecular Weight

143.10

Formula

C3H5N5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C(N)C1=NNN=N1

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 : 5 mg/mL (34.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.9881 mL 34.9406 mL 69.8812 mL
5 mM 1.3976 mL 6.9881 mL 13.9762 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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In Vivo Dissolution Calculator
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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
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 6.9881 mL 34.9406 mL 69.8812 mL 174.7030 mL
5 mM 1.3976 mL 6.9881 mL 13.9762 mL 34.9406 mL
10 mM 0.6988 mL 3.4941 mL 6.9881 mL 17.4703 mL
15 mM 0.4659 mL 2.3294 mL 4.6587 mL 11.6469 mL
20 mM 0.3494 mL 1.7470 mL 3.4941 mL 8.7351 mL
25 mM 0.2795 mL 1.3976 mL 2.7952 mL 6.9881 mL
30 mM 0.2329 mL 1.1647 mL 2.3294 mL 5.8234 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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(RS)-(Tetrazol-5-yl)glycine
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