MRS-1706

SKU: orb1218249

Description

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

Key Properties

• CAS Number: 264622-53-9
• MW: 503.55
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₉N₅O₅
• SMILES: O=C(NC1=CC=C(C(C)=O)C=C1)COC2=CC=C(C3=NC(N(CCC)C(N(CCC)C4=O)=O)=C4N3)C=C2
• Target: Adenosine Receptor
• Solubility: DMSO:6.4 mg/mL (12.71 mM; Need ultrasonic and warming);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• In Vivo:
  MRS-1706 (1-10 μM; intracavernous injection; Ada–/– mice) reduces the magnitude and duration of electrical field stimulation (EFS)-induced contraction of corpus cavernosal strips (CCSs) from sickle cell disease (SCD) transgenic mice and inhibits the level of cAMP. Animal model: Ada–/–mice. Dosage: 1 and 10 μM. Administration: Intracavernous injection. Result: Inhibited A2BR signaling and reduced the magnitude and duration. Inhibited the level of cAMP.
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• In Vitro:
  MRS-1706 (0.1-5 μM) has antagonist effect of NECA on the wild-type adenosine A2B receptor in a dose-dependent manner. MRS-1706 (0.1-10000 nM) induces inhibition of yeast growth, which yeast cells expressing seven CAM adenosine A2B receptors, with IC50 values of 43, 54, 40, 98, 166, 133 nM for F84 L, F84S, F84 L/S95G, T42A, T42A/V54A, N36S/T42A, respectively. MRS-1706 (1 μM) inhibits the adenosine-mediated induction of cAMP in wild-type corpus cavernosal strips (CCSs) and decreases the level of cAMP.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Adenosine Receptor