2. Immunology/Inflammation
  3. NTPDase
  4. ARL67156 trisodium

ARL67156 trisodium  (Synonyms: FPL 67156 trisodium)

Cat. No.: HY-103265 Purity: 99.8%
COA Handling Instructions

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ARL67156 trisodium salt est un inhibiteur de l'ecto-ATPase. ARL67156 trisodium salt est un inhibiteur compétitif faible de NTPDase1 (CD39), NTPDase3 et NPP1, avec des Ki de 11, 18 et 12 μM, respectivement. ARL67156 trisodium salt empêche le développement in vivo de la maladie de la valve aortique calcifiante.

ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.

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

ARL67156 trisodium Chemical Structure

ARL67156 trisodium Chemical Structure

CAS No. : 1021868-83-6

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Based on 2 publication(s) in Google Scholar

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ARL67156 trisodium Related Antibodies

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Description

ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma[1][2].

IC50 & Target

Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]; 0.97 μM (CD39), 0.45 μM (CD73)[8]
In Vitro

ARL67156 trisodium (1-100 μM) potentiates neurogenic contractions in a concentration-dependent manner[4].
? ARL67156 trisodium (10 μg/mL, 24 h) increases the surface expression of CXCR3 on ATP-treated HMC-1 cells[5].
? ARL67156 trisodium (30 μM, 5s) potentiates the norepinephrine release promoted by ATP in guinea pig heart synaptosomes[6].
? ARL67156 trisodium (100 μM, 4h) significantly decreases HIV-1replication in macrophages[7].

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

ARL67156 trisodium Related Antibodies
In Vivo

ARL67156 trisodium (1.1 μg/kg/day, administered with osmotic pumps implanted subcutaneously, for 28 days) prevents the development of calcific aortic valve disease in Warfarin (HY-B0687)-treated rats[2].
? ARL67156 trisodium (intraperitoneal injection, 2?mg/kg) prevents the increase of serum adenosine concentration induced by Fructose 1,6-bisphosphate (FBP)[3].

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

Animal Model: Warfarin-induced mineralization rat model[2]
Dosage: 1.1 μg/kg/day
Administration: Administered with osmotic pumps implanted subcutaneously, for 28 days
Result: Prevented the development of aortic stenosis by lowering the level of apoptosis and mineralization of the aortic valve/aorta.
Normalized the level of pAkt (an important kinase involved in the survival pathway).
Animal Model: C57BL/6 mice[3]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection, 1  h before administration of FBP (100 mg/kg)
Result: Completely abolished the anti-inflammatory effects of FBP (observed by the neutrophil infiltration, hyperalgesia and oedema of the joint).
Molecular Weight

785.05

Formula

C15H21Br2N5Na3O12P3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@H](O[C@H](COP(OP(C(Br)(Br)P(O)(O[Na])=O)(O[Na])=O)(O[Na])=O)[C@H]1O)N2C3=NC=NC(N(CC)CC)=C3N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (31.85 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2738 mL 6.3690 mL 12.7380 mL
5 mM 0.2548 mL 1.2738 mL 2.5476 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). 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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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
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: 99.8%

COA (260 KB) Elemental Analysis Report (118 KB)

Handling Instructions (2659 KB)
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). 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 1.2738 mL 6.3690 mL 12.7380 mL 31.8451 mL
5 mM 0.2548 mL 1.2738 mL 2.5476 mL 6.3690 mL
10 mM 0.1274 mL 0.6369 mL 1.2738 mL 3.1845 mL
15 mM 0.0849 mL 0.4246 mL 0.8492 mL 2.1230 mL
20 mM 0.0637 mL 0.3185 mL 0.6369 mL 1.5923 mL
25 mM 0.0510 mL 0.2548 mL 0.5095 mL 1.2738 mL
30 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0615 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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ARL67156 trisodium Related Classifications

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  • 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:

ARL67156 trisodium1021868-83-6FPL 67156 trisodiumNTPDaseEcto-ATPaseEctonucleotidaseFBPASMCcalcific aorticATPasthmaInhibitorinhibitorinhibit

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