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

OP-5244 sodium is a potent and orally active 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
10 mg USD 1400 In-stock
25 mg USD 2950 In-stock
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Based on 1 publication(s) in Google Scholar

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OP-5244 sodium Related Antibodies

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Description

OP-5244 sodium is a potent and orally active 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].

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

OP-5244 sodium Related Antibodies
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].

MedChemExpress (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
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@H](O)[C@H](N2N=CC3=C(NC4CCCC4)N=C(Cl)N=C32)O[C@@H]1CO[C@]([P](O)(O[Na])=O)(COC)CO
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)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (59.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7861 mL 8.9306 mL 17.8613 mL
5 mM 0.3572 mL 1.7861 mL 3.5723 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7861 mL 8.9306 mL 17.8613 mL 44.6532 mL
5 mM 0.3572 mL 1.7861 mL 3.5723 mL 8.9306 mL
10 mM 0.1786 mL 0.8931 mL 1.7861 mL 4.4653 mL
15 mM 0.1191 mL 0.5954 mL 1.1908 mL 2.9769 mL
20 mM 0.0893 mL 0.4465 mL 0.8931 mL 2.2327 mL
25 mM 0.0714 mL 0.3572 mL 0.7145 mL 1.7861 mL
30 mM 0.0595 mL 0.2977 mL 0.5954 mL 1.4884 mL
40 mM 0.0447 mL 0.2233 mL 0.4465 mL 1.1163 mL
50 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8931 mL
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OP-5244 sodium Related Classifications

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.

Keywords:

OP-5244OP5244OP 5244CD73ecto-5′-nucleotidase, NT5EimmunosuppressionadenosinecancerInhibitorinhibitorinhibit

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