A short-acting A2A receptor agonist
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Regadenoson

Item No. 18814

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]-adenosine
CAS Number
313348-27-5
Synonyms
  • CVT-3146
  • Lexiscan
Molecular Formula
C15H18N8O5
Formula Weight
390.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 14 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
247, 271 nm
SMILES
O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=C(N4N=CC(C(NC)=O)=C4)N=C3N)O[C@@H]1CO
InChi Code
InChI=1S/C15H18N8O5/c1-17-13(27)6-2-19-23(3-6)15-20-11(16)8-12(21-15)22(5-18-8)14-10(26)9(25)7(4-24)28-14/h2-3,5,7,9-10,14,24-26H,4H2,1H3,(H,17,27)(H2,16,20,21)/t7-,9-,10-,14-/m1/s1
InChi Key
LZPZPHGJDAGEJZ-AKAIJSEGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $154

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    10 mg

    $259

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    25 mg

    $527

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    Product Description

    Regadenoson is a selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor).1,2 It increases coronary blood flow 3.4- to 3.8-fold with a half-time to reversal of 1.9-2.6 minutes in open-chest anesthetized pigs.1 Regadenoson is used to induce hyperemia (increased blood flow), particularly in the context of myocardial perfusion imaging.3,4 It has also been found to increase the delivery of compounds to the central nervous system through the blood-brain barrier in animals.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gao, Z., Li, Z., Baker, S.P., et al. Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: Inverse relationship between affinity and duration of action of A2A agonists. J. Pharmacol. Exp. Ther. 298(1), 209-218 (2001).

    2. Zhao, G., Linke, A., Xu, X., et al. Comparative profile of vasodilation by CVT-3146, a novel A2A receptor agonist, and adenosine in conscious dogs. J. Pharmacol. Exp. Ther. 307(1), 182-189 (2003).

    3. Bhatti, S., Hakeem, A., Dhanalakota, S., et al. Prognostic value of regadenoson myocardial single-photon emission computed tomography in patients with different degrees of renal dysfunction. Eur.Heart J.Cardiovasc.Imaging 15(8), 933-940 (2014).

    4. Verberne, H.J., Acampa, W., Anagnostopoulos, C., et al. EANM procedural guidelines for radionuclide myocardial perfusion imaging with SPECT and SPECT/CT: 2015 revision. Eur. J. Nucl. Med. Mol. Imaging 42(12), 1929-1940 (2015).

    5. Carman, A.J., Mills, J.H., Krenz, A., et al. Adenosine receptor signaling modulates permeability of the blood-brain barrier. J. Neurosci. 31(37), 13272-13280 (2011).

    6. Jackson, S., Anders, N.M., Mangraviti, A., et al. The effect of regadenoson-induced transient disruption of the blood-brain barrier on temozolomide delivery to normal rat brain. J. Neurooncol. 126(3), 433-439 (2016).