| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]
NTPDase1 (CD39), NTPDase3, and NPP1. ARL67156 competitively inhibits these ectonucleotidases with Ki values of 11 uM (NTPDase1), 18 uM (NTPDase3), and 12 uM (NPP1), thereby preventing the hydrolysis of extracellular ATP and ADP. |
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| ln Vitro |
Concentration-dependent neurogenic contractions are amplified by ARL67156 trisodium hydrate (1-100 μM)[4]. The surface expression of CXCR3 on ATP-treated HMC-1 cells is increased by ARL67156 trisodium hydrate (10 μg/mL, 24 h)[5]. Norepinephrine production in guinea pig cardiac synaptosomes stimulated by ATP is amplified by ARL67156 trisodium hydrate (30 μM, 5s)[6]. In macrophages, ARL67156 trisodium hydrate (100 μM, 4h) dramatically reduces HIV-1 replication[7].
In vitro, ARL67156 inhibits UTP breakdown in superior cervical ganglion cells and potentiates nucleotide-induced contractions in isolated rat tail artery. It is not an effective inhibitor of NTPDase2, NTPDase8, NPP3, or ecto-5'-nucleotidase (CD73). |
| ln Vivo |
In rats treated with Warfarin (HY-B0687), ARL67156 trisodium hydrate (1.1 μg/kg/day) inhibits the development of calcific aortic valve disease when supplied with subcutaneously implanted osmotic pumps for 28 days[2]. The intraperitoneal injection of ARL67156 trisodium hydrate (2 mg/kg) inhibits the rise in blood adenosine concentration brought on by fructose 1,6-bisphosphate (FBP)[3].
ARL67156 prevents the development of calcific aortic valve disease in vivo, indicating its role in modulating purinergic signaling in disease models. It has been shown to potentiate UTP- and ATP-induced responses in isolated tissue preparations. |
| Enzyme Assay |
Enzyme activity assays use membrane preparations from human or mouse origin expressing recombinant NTPDases. The compound is incubated with ATP or ADP as substrate. Released inorganic phosphate is quantified by colorimetric methods, or residual ATP is measured by luciferin/luciferase assay. Ki values are calculated from Lineweaver-Burk plots.
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| Cell Assay |
Not typically used for live-cell functional assays as a primary endpoint. May be added to cell culture media at concentrations of 10-100 uM to inhibit ecto-ATPase activity in intact cells. Inhibition is confirmed by measuring ATP levels in culture supernatants or by assaying cell lysates for enzyme activity.
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| Animal Protocol |
Animal/Disease Models: Warfarin-induced mineralization rat model[2]
Doses: 1.1 μg/kg/day Route of Administration: Administered with osmotic pumps implanted subcutaneously (sc), for 28 days Experimental Results: 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/Disease Models: C57BL/6 mice[3] Doses: 2 mg/kg Route of Administration: intraperitoneal (ip)injection, 1 h before administration of FBP (100 mg/kg) Experimental Results: Completely abolished the anti-inflammatory effects of FBP (observed by the neutrophil infiltration, hyperalgesia and oedema of the joint). In mouse models of calcific aortic valve disease, ARL67156 is administered via intraperitoneal injection (dosing regimen not standardized). Disease progression is monitored by histopathological examination of valve sections for calcification, and by molecular analysis of inflammatory and osteogenic markers in valve tissue. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data available. As a small-molecule nucleotide analog, it is likely to have limited oral bioavailability and rapid systemic clearance. For research use, it is typically formulated in saline or PBS and administered via injection for in vivo studies.
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| Toxicity/Toxicokinetics |
No detailed toxicological data reported in the literature. At concentrations used for NTPDase inhibition (10-100 uM in vitro, and corresponding doses in vivo), no severe cytotoxicity or systemic toxicity has been described. Standard safety precautions for handling nucleotide derivatives apply.
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| References |
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| Additional Infomation |
ARL67156 is also known as FPL 67156. It is a selective but weak inhibitor of NTPDases, with limited selectivity among family members. It is not FDA-approved and is strictly for research use in studying purinergic signaling, inflammation, and diseases involving ectonucleotidases.
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| Molecular Formula |
C15H23BR2N5NA3O13P3
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|---|---|
| Molecular Weight |
834.61
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| Related CAS # |
ARL67156 trisodium;1021868-83-6;ARL67156 triethylamine
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1982 mL | 5.9908 mL | 11.9816 mL | |
| 5 mM | 0.2396 mL | 1.1982 mL | 2.3963 mL | |
| 10 mM | 0.1198 mL | 0.5991 mL | 1.1982 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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