| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Ki: 11 μM (NTPDase1), 18 μM (NTPDase3), 12 μM (NPP1)[1]
The primary targets of ARL 67156 trisodium are ecto-nucleotidases, including NTPDase1 (CD39), NTPDase3, and NPP1. These enzymes hydrolyze extracellular nucleotides such as ATP and ADP, thereby regulating purinergic signaling. ARL 67156 acts as a weak competitive inhibitor of these enzymes, with Ki values of 11 μM for NTPDase1 (CD39), 18 μM for NTPDase3, and 12 μM for NPP1. By inhibiting ecto-nucleotidases, the compound increases the concentration of extracellular ATP, which can modulate immune responses and other cellular functions. |
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| ln Vitro |
In a concentration-dependent manner, ARL67156 trisodium (1-100 μM) improves neurogenic contractions [4]. On the cell membrane surface of ATP-treated HMC-1 cells, ARL67156 trisodium (10 μg/mL, 24 h) increases the expression of CXCR3 [5]. The release of norepinephrine in guinea pig cardiac synaptosomes stimulated by ATP is improved by ARL67156 trisodium (30 μM, 5s) [6]. Significantly less HIV-1 replication occurs in macrophages when treated with ARL67156 trisodium (100 μM, 4h) [7].
In vitro, ARL 67156 trisodium demonstrates inhibitory activity against ecto-nucleotidases. Its activity is assessed in enzyme assays using recombinant or native NTPDase enzymes and ATP or ADP as substrates. The compound shows weak competitive inhibition, with Ki values of 11 μM for NTPDase1 (CD39), 18 μM for NTPDase3, and 12 μM for NPP1. It also inhibits ecto-ATPase activity. However, detailed cellular activity data are not extensively reported in the available literature. |
| ln Vivo |
Trisodium, ARL67156 (1.1 μg/kg/day, subcutaneous inlet osmotic pump for 28 days), protects warfarin-treated deposits against calcific aortic valve damage [2]. Increases in blood adenosine concentrations caused by fructose-1,6-bisphosphate (FBP) can be avoided by ARL67156 trisodium (intraperitoneal injection, 2 mg/kg) [3].
In vivo data for ARL 67156 trisodium are limited in the available literature. Based on its immunomodulatory and anticancer activity, the compound has potential for in vivo applications. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical. |
| Enzyme Assay |
In vitro enzyme assays for ARL 67156 trisodium typically involve measuring its inhibitory activity against ecto-nucleotidases such as NTPDase1 (CD39), NTPDase3, and NPP1. The enzyme is incubated with a nucleotide substrate (e.g., ATP or ADP) in the presence of varying concentrations of the compound. The hydrolysis of the nucleotide to its corresponding monophosphate (AMP or ADP) is measured, and the rate of hydrolysis is determined. The inhibition constant (Ki) is calculated from the enzyme kinetics in the presence of different inhibitor concentrations.
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| Cell Assay |
Cellular assays for ARL 67156 trisodium are performed in various cell types to assess its effects on purinergic signaling. Cells are treated with the compound, and the levels of extracellular ATP or other nucleotides are measured. The compound's effects on cellular functions such as immune cell activation, proliferation, or apoptosis are also assessed. These assays are used to study the role of ecto-nucleotidases in cellular physiology.
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| Animal Protocol |
Animal/Disease Models: Warfarin-induced mineralization rat model [2]
Doses: 1.1 μg/kg/day Route of Administration: Osmotic administration subcutaneously (sc) (sc) implanted pump for 28 days Experimental Results: By lowering the aortic valve/aorta levels of apoptosis and mineralization to prevent the development of aortic stenosis. Normalization of levels of pAkt, an important kinase involved in survival pathways. Animal/Disease Models: C57BL/6 mice [3] Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection 1 hour before administration of FBP (100 mg/kg) Experimental Results: Complete elimination of the anti-inflammatory effect of FBP (via neutrophils Infiltration observation), hyperalgesia and joint edema). In vivo animal studies with ARL 67156 trisodium are not extensively documented in the available literature. Based on its immunomodulatory and anticancer activity, potential in vivo models could include tumor models or models of inflammatory diseases. In such studies, ARL 67156 trisodium would be administered intraperitoneally or intravenously. However, specific protocols are not detailed in the available sources. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for ARL 67156 trisodium are not extensively reported. As an ATP analog, the compound is expected to have limited oral bioavailability and may require parenteral administration for in vivo studies. It is typically dissolved in DMSO or aqueous buffers for in vitro studies. However, detailed pharmacokinetic parameters such as half-life, clearance, and volume of distribution are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for ARL 67156 trisodium are not extensively reported. As a nucleotide analog, it may have effects on nucleotide metabolism and purinergic signaling that could contribute to toxicity at high concentrations. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
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| Additional Infomation |
ARL 67156 trisodium is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying ecto-nucleotidases and purinergic signaling. The compound is used to investigate the role of CD39 and other ecto-nucleotidases in immune regulation, inflammation, and cancer. It is also used to study the effects of extracellular ATP on cellular function.
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| Molecular Formula |
C15H21BR2N5O12P3
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|---|---|
| Molecular Weight |
716.082824468613
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| Exact Mass |
784.843
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| CAS # |
1021868-83-6
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| Related CAS # |
ARL67156 trisodium hydrate;ARL67156 triethylamine
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| PubChem CID |
11957464
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
40
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| Complexity |
941
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O[C@H]1[C@@H](O[C@H](COP(OP(C(Br)(Br)P(O)(O)=O)(O)=O)(O)=O)[C@H]1O)N2C3=NC=NC(N(CC)CC)=C3N=C2.[3Na]
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| InChi Key |
KJYSFRKUFDOOSQ-TZRPAKANSA-K
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| InChi Code |
InChI=1S/C15H24Br2N5O12P3.3Na/c1-3-21(4-2)12-9-13(19-6-18-12)22(7-20-9)14-11(24)10(23)8(33-14)5-32-37(30,31)34-36(28,29)15(16,17)35(25,26)27;;;/h6-8,10-11,14,23-24H,3-5H2,1-2H3,(H,28,29)(H,30,31)(H2,25,26,27);;;/q;3*+1/p-3/t8-,10-,11-,14-;;;/m1.../s1
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| Chemical Name |
[dibromo-[[[(2R,3S,4R,5R)-5-(6-diethylaminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid
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| Synonyms |
ARL-67156 FPL-67156 ARL67156FPL67156 ARL 67156
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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) |
H2O : ~25 mg/mL (~31.85 mM)
DMSO : ~1 mg/mL (~1.27 mM) |
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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 | 1.3965 mL | 6.9825 mL | 13.9649 mL | |
| 5 mM | 0.2793 mL | 1.3965 mL | 2.7930 mL | |
| 10 mM | 0.1396 mL | 0.6982 mL | 1.3965 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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