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  2. Drug Derivative mGluR
  3. Talaglumetad (hydrochloride)

Talaglumetad (hydrochloride)  (Synonyms: LY-544344 (hydrochloride))

Cat. No.: HY-131286A Purity: 99.58%
Handling Instructions Technical Support

Talaglumetad hydrochloride (LY-544344 hydrochloride) is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad hydrochloride undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad hydrochloride can be used in research related to metabotropic glutamate receptor 2-associated neurological systems.

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

Talaglumetad (hydrochloride)

Talaglumetad (hydrochloride) Chemical Structure

CAS No. : 441765-97-5

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Based on 1 publication(s) in Google Scholar

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Description

Talaglumetad hydrochloride (LY-544344 hydrochloride) is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad hydrochloride undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad hydrochloride can be used in research related to metabotropic glutamate receptor 2-associated neurological systems[1][2].

IC50 & Target[2]

mGluR2

 

mGluR3

 

Cellular Effect
Cell Line Type Value Description References
Caco-2 IC50
0.3 mM
Compound: 12a
Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into Caco-2 cells done for 15 min at 37 degree C with compound
Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into Caco-2 cells done for 15 min at 37 degree C with compound
[PMID: 16078848]
In Vitro

Talaglumetad (LY-544344) hydrochloride functions as a substrate for the intestinal peptide transporter hPepT1 and is readily hydrolyzed by rat and human jejunum S9 fractions and plasma in vitro[2].

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

In Vivo

Talaglumetad (LY-544344) hydrochloride (p.o.) increases systemic exposure to the parent drug LY-354740 by up to 17-fold in healthy rats, with negligible prodrug levels in circulation[2].
Talaglumetad hydrochloride (p.o.) increases systemic exposure to the parent drug LY-354740 by up to 16-fold in healthy dogs, with negligible prodrug levels in circulation and dose-proportional parent drug exposure[2].

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

Molecular Weight

292.72

Formula

C11H17ClN2O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H](N)C)N[C@]([C@@]1([H])[C@]2([H])[C@@H]1C(O)=O)(CC2)C(O)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 1.25 mg/mL (4.27 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4162 mL 17.0812 mL 34.1623 mL
5 mM --- --- ---
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 (sealed storage, away from moisture). 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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Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 3.4162 mL 17.0812 mL 34.1623 mL 85.4058 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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    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.

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Product Name:
Talaglumetad (hydrochloride)
Cat. No.:
HY-131286A
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