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

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.

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TC-N 22A

TC-N 22A 構造式

CAS 番号 : 1314140-00-5

容量 価格（税別） 在庫状況 数量
1 mg $375 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
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10 mg   お問い合わせ  
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TC-N 22A 関連抗体

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製品説明

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]
体外実験

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].

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

TC-N 22A 関連抗体
体内実験

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].

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

283.35

分子式

C14H13N5S
CAS 番号
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
溶剤 & 溶解度

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The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

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

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TC-N 22A Related Classifications

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Help & FAQs
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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.

Keywords:

TC-N 22A1314140-00-5mGluRMetabotropic glutamate receptorsPAMBHK cellCNS diseasemGlu4Inhibitorinhibitorinhibit

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