1. GPCR/G Protein
  2. Adenosine Receptor
  3. Adenosine receptor inhibitor 1

Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.

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Adenosine receptor inhibitor 1 Chemical Structure

Adenosine receptor inhibitor 1 Chemical Structure

CAS No. : 2550400-52-5

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Description

Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].

IC50 & Target[1]

A1AR

>1000 nM (Ki)

A2AR

68.5 nM (Ki)

hA2B

>1000 nM (Ki)

Adenosine A3 receptor

>1000 nM (Ki)

In Vitro

Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively[1].

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

In Vivo

Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner[1].
Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model[1].
Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse[1].

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

Animal Model: 18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin) [1]
Dosage: 20, 30, 40 mg/kg
Administration: I.p.
Result: Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus.
Animal Model: 150-180 g male rats Wistar(carrageenan-induced edema model)[1]
Dosage: 20 mg/kg
Administration: I.p.
Result: Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively.
Animal Model: Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.p.
Result: Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.
Molecular Weight

395.82

Formula

C17H19ClFN5O3

CAS No.
SMILES

O=C(N1CC)N(C)C2=C(N(C)C(NCC3=C(Cl)C=CC(OC)=C3F)=N2)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Adenosine receptor inhibitor 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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Adenosine receptor inhibitor 1
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HY-147907
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