1. Immunology/Inflammation
  2. NTPDase CD73
  3. 8-BuS-AMP

8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC50 of 35 μM and a Ki value of 0.292 μM against human NTPDase1; its Ki values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies.

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8-BuS-AMP

8-BuS-AMP Chemical Structure

CAS No. : 344402-39-7

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Description

8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC50 of 35 μM and a Ki value of 0.292 μM against human NTPDase1; its Ki values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies[1][2][3].

In Vitro

8-BuS-AMP (100 μM; 10 min) impairs recombinant human NTPDase1's ability to inhibit ADP-induced platelet aggregation, but does not itself induce or inhibit platelet aggregation, indicating in vitro inactivity towards platelet P2Y1 and P2Y12 receptors[2].
8-BuS-AMP (1 μM; 0, 20, 40, 60 min) is highly metabolically stable in human and mouse liver microsomes, with half-lives of 462 min and 182 min, respectively[3].
8-BuS-AMP (1-100 μM; 1 h) concentration-dependently inhibits nucleotide hydrolysis in human synovial fluid, reducing adenosine formation from both ε-ATP and ε-AMP[3].
8-BuS-AMP (10-100 μM; 3 days, added daily) concentration-dependently enhances activation (via increased CD25 expression) and proliferation of human primary CD4+ and CD8+ T lymphocytes without reducing cell viability[3].

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

In Vivo

8-BuS-AMP (100 μM; added to histochemical reaction buffer) specifically inhibits NTPDase1-mediated ATPase activity in mouse liver vascular tissues without affecting NTPDase activity in kidney tubules[2].

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

Molecular Weight

435.39

Formula

C14H22N5O7PS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@H](O)[C@H](N2C(N=CN=C3N)=C3N=C2SCCCC)O[C@@H]1COP(O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (114.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2968 mL 11.4840 mL 22.9679 mL
5 mM 0.4594 mL 2.2968 mL 4.5936 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.90%

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. 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
H2O 1 mM 2.2968 mL 11.4840 mL 22.9679 mL 57.4198 mL
5 mM 0.4594 mL 2.2968 mL 4.5936 mL 11.4840 mL
10 mM 0.2297 mL 1.1484 mL 2.2968 mL 5.7420 mL
15 mM 0.1531 mL 0.7656 mL 1.5312 mL 3.8280 mL
20 mM 0.1148 mL 0.5742 mL 1.1484 mL 2.8710 mL
25 mM 0.0919 mL 0.4594 mL 0.9187 mL 2.2968 mL
30 mM 0.0766 mL 0.3828 mL 0.7656 mL 1.9140 mL
40 mM 0.0574 mL 0.2871 mL 0.5742 mL 1.4355 mL
50 mM 0.0459 mL 0.2297 mL 0.4594 mL 1.1484 mL
60 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9570 mL
80 mM 0.0287 mL 0.1435 mL 0.2871 mL 0.7177 mL
100 mM 0.0230 mL 0.1148 mL 0.2297 mL 0.5742 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Product Name:
8-BuS-AMP
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HY-173447
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