1. Immunology/Inflammation
  2. CD73
  3. OP-5244 sodium

OP-5244 sodium 

Cat. No.: HY-136978A
Handling Instructions

OP-5244 sodium is a potent and orally bioavailable inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.

For research use only. We do not sell to patients.

OP-5244 sodium Chemical Structure

OP-5244 sodium Chemical Structure

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5 mg USD 850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

OP-5244 sodium is a potent and orally bioavailable inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].

IC50 & Target

IC50: 0.25 nM (CD73)[1]

In Vitro

OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells[1].
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8+ T cells with an EC50 of 0.22 nM[1].
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8+ T cells proliferation and cytokine production[1].
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively)[1].

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

In Vivo

OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1].
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) [1].

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

Animal Model: BALB/c mice with breast cancer[1]
Dosage: 15 mg/kg/day
Administration: S.c. for 13 days
Result: Inhibited tumor growth.
Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group.
Molecular Weight

559.87

Formula

C₁₉H₂₈ClN₅NaO₉P

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

References
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OP-5244 sodium
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HY-136978A
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