An OX2R antagonist (Ki = 1.1 nM); selective for OX2R over OX1R (Ki = 900 nM); inhibits orexin-A- and orexin-B-induced calcium mobilization (IC50s = 8.8 and 7.9 nM

EMPA – 10 mg

Brand:
Cayman
CAS:
680590-49-2
Storage:
-20
UN-No:
Non-Hazardous - /

EMPA is an orexin 2 receptor (OX2R) antagonist (Ki = 1.1 nM).{45690} It is selective for OX2R over OX1R (Ki = 900 nM). EMPA inhibits orexin-A- and orexin-B-induced calcium mobilization (IC50s = 8.8 and 7.9 nM, respectively) and increases orexin-A- and orexin-B-induced inositol phosphate accumulation (EC50s = 1.1 and 2.4 nM, respectively) in CHO(dHFr-) cells expressing recombinant human OX2R. It reduces spontaneous locomotor activity and orexin-B-induced hyperlocomotion in mice when administered at doses ranging between 10 and 300 mg/kg.  

 

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SKU: 29446 - 10 mg Category:

Description

An OX2R antagonist (Ki = 1.1 nM); selective for OX2R over OX1R (Ki = 900 nM); inhibits orexin-A- and orexin-B-induced calcium mobilization (IC50s = 8.8 and 7.9 nM, respectively) and increases orexin-A- and orexin-B-induced inositol phosphate accumulation (EC50s = 1.1 and 2.4 nM, respectively) in CHO(dHFr-) cells expressing recombinant human OX2R; reduces spontaneous locomotor activity and orexin-B-induced hyperlocomotion in mice at 10-300 mg/kg

Formal name: N-ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide

Synonyms: 

Molecular weight: 454.5

CAS: 680590-49-2

Purity: ≥98%

Formulation: An oil

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