An adenosine A2B receptor antagonist; selective for adenosine A2B receptors over A1

BAY-545 – 5 mg

Brand:
Cayman
CAS:
1699717-32-2
Storage:
-20
UN-No:
Non-Hazardous - /

BAY-545 is an adenosine A2B receptor antagonist.{50105} It is selective for adenosine A2B receptors over A1, A2A, and A3 receptors with IC50 values of 66, 1,300, 820, and >6,700 nM, respectively, in CHO cell membranes expressing human recombinant receptors. BAY-545 reduces increases in the levels of IL-6 induced by the adenosine receptor agonist 5′-(N-ethylcarbamoyl)adenosine (NECA; Item No. 21420) in LL29 fibroblast cells (IC50 = 185 nM). It decreases FITC-induced increases in the levels of IL-6 in lung homogenates and cell numbers in bronchoalveolar lavage fluid (BALF) and reduces silica-induced increases in the levels of TGF-β1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis when administered at a dose of 500 mg/kg.  

 

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SKU: 28420 - 5 mg Category:

Description

An adenosine A2B receptor antagonist; selective for adenosine A2B receptors over A1, A2A, and A3 receptors (IC50s = 66, 1,300, 820, and >6,700 nM, respectively); reduces increases in the levels of IL-6 induced by the adenosine receptor agonist NECA in LL29 fibroblast cells (IC50 = 185 nM); decreases FITC-induced increases in the levels of IL-6 in lung homogenates and cell numbers in BALF and reduces silica-induced increases in the levels of TGF-β1 in lung homogenates, but not cell numbers in BALF, in mouse models of pulmonary fibrosis at 500 mg/kg

Formal name: 3-ethyl-6-[(4-hydroxy-1-piperidinyl)carbonyl]-5-methyl-1-(3,3,3-trifluoropropyl)-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione

Synonyms: 

Molecular weight: 433.4

CAS: 1699717-32-2

Purity: ≥95%

Formulation: A solid

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