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TCN238

Catalog No. T7494 CAS 125404-04-8

Synonyms: TCN 238

TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM).

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TCN238, CAS 125404-04-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 186.00
50 mg	In stock	$ 320.00
100 mg	In stock	$ 555.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Storage & Solubility Information

Description	TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM).
Targets&IC50	mGlu4 receptor:1 μM (EC50)
In vitro	TCN238 has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells[1].
In vivo	TCN238 has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 μM.?In a haloperidol-induced catalepsy rat model of Parkinson's disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg.?TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory[1].

Synonyms	TCN 238
Molecular Weight	197.24
Formula	C12H11N3
CAS No.	125404-04-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (760.49 mM)

References and Literature

1. Pershina E V , Arkhipov V I . Subacute activation of mGlu4 receptors causes the feedback inhibition of its gene expression in rat brain[J]. Life Sciences, 2016, 153:50-54. 2. East S P , Bamford S , Dietz M G A , et al. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20(16):4901-4905.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library NO PAINS Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Orally Active Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

TCN238 125404-04-8 Neuroscience GluR inhibit TCN-238 mGluR Metabotropic glutamate receptors TCN 238 Inhibitor inhibitor

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