1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. TC-N 22A

TC-N 22A 

Cat. No.: HY-18679
Handling Instructions

TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.

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

TC-N 22A Chemical Structure

TC-N 22A Chemical Structure

CAS No. : 1314140-00-5

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Description

TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo[1].

IC50 & Target

EC50: 9 nM (mGlu4 receptor)
EC50: >10 μM (mGlu 1, 2, 3, 5, and 7 receptors)[1]

In Vitro

TC-N 22A is selected for mGlu4 and has an EC50 of 9 nM in human mGlu4-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC50>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC50 >10 μM) and shows low potential for hERG channel inhibition[1].

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

In Vivo

TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats[1].

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

Molecular Weight

283.35

Formula

C₁₄H₁₃N₅S

CAS No.

1314140-00-5

SMILES

C1(NC2=NC3=C(CCCC4=NNC=C43)S2)=CC=CC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vivo:
  • 1.

    TC-N 22A is suspended in 20% aqueous hydroxypropyl β-cyclodextrin[1].

References
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Keywords:

TC-N 22AmGluRMetabotropic glutamate receptorsPAMBHK cellCNS diseasemGlu4Inhibitorinhibitorinhibit

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TC-N 22A
Cat. No.:
HY-18679
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