| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
PSB-12379 targets ecto-5'-nucleotidase (CD73), a membrane-bound enzyme that catalyzes the hydrolysis of extracellular AMP to adenosine. CD73 is a key enzyme in the purinergic signaling pathway, converting AMP to adenosine, which then activates adenosine receptors. PSB-12379 is a potent inhibitor of CD73, with Kis of 9.03 nM (rat) and 2.21 nM (human). By inhibiting CD73, PSB-12379 prevents the production of adenosine, thereby modulating purinergic signaling.
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| ln Vitro |
Consumption: After 8 hours of sustained loading, only a tiny portion (<23%) of PSB-12379 (10g) was consumed under application conditions. However, >77% of the compound remained unaltered. The 10g of PSB-12379 is a little unstable; after 8 hours, 56% of it was gone. The nuclear sequence is the arrangement of sugar sequence bonds, and the usual I substitution at the top is seen to be the dominant reaction [1].
In vitro, PSB-12379 is a potent inhibitor of CD73, with Kis of 9.03 nM (rat) and 2.21 nM (human). It blocks ecto-5'-nucleotidase-mediated adenosine production by preventing the conversion of AMP to adenosine. It exhibits selectivity over other ecto-nucleotidases and ADP-activated P2Y receptors tested. PSB-12379 represents the most potent eN inhibitor known to date, showing high selectivity and metabolic stability. |
| ln Vivo |
In vivo, PSB-12379 is used to study adenosine-mediated signaling in inflammation, fibrosis, and cancer biology. By inhibiting CD73, it can modulate purinergic signaling and affect various physiological and pathological processes. However, specific in vivo protocols and results are not detailed in standard product descriptions. PSB-12379 is a research tool for studying CD73 and purinergic signaling.
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| Enzyme Assay |
In vitro enzyme assays for PSB-12379 measure its inhibition of CD73 (ecto-5'-nucleotidase) activity. CD73 enzyme is incubated with AMP substrate in the presence of varying concentrations of PSB-12379. The production of adenosine and inorganic phosphate is measured, and the Ki is determined from the dose-response curve. Selectivity is assessed by testing the compound against other ecto-nucleotidases.
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| Cell Assay |
In vitro cell-based assays for PSB-12379 are used to study its effects on adenosine production and purinergic signaling. Cells expressing CD73 are treated with PSB-12379, and the conversion of AMP to adenosine is measured by HPLC or using a fluorescent adenosine sensor. The compound's effects on downstream signaling pathways, such as cAMP accumulation or calcium mobilization, can also be assessed. These assays confirm the compound's cellular activity as a CD73 inhibitor.
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| Animal Protocol |
In vivo animal experiments for PSB-12379 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a CD73 inhibitor would involve its administration to animal models of cancer, inflammation, or fibrosis. However, specific protocols for PSB-12379 are not detailed.
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| ADME/Pharmacokinetics |
PSB-12379 disodium has a molecular weight not specified in standard product descriptions. It is a solid compound. It is soluble in water and organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PSB-12379 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. PSB-12379 is a CD73 inhibitor, and its toxicity would be related to its effects on purinergic signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
PSB-12379 disodium is a research compound and is not approved for any clinical or therapeutic use. It is a potent inhibitor of ecto-5'-nucleotidase (CD73). PSB-12379 is an α,β-Methylene-ADP (AOPCP) derivative. It inhibits CD73 with Kis of 9.03 nM (rat) and 2.21 nM (human). PSB-12379 blocks CD73-mediated adenosine production and exhibits selectivity over other ecto-nucleotidases. It is used to study adenosine-mediated signaling in inflammation, fibrosis, and cancer biology.
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| Molecular Formula |
C18H23N5O9P2
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|---|---|
| Molecular Weight |
515.3508
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| Exact Mass |
515.097
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| CAS # |
1802226-78-3
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| Related CAS # |
PSB-12379 disodium
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| PubChem CID |
122207761
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| Appearance |
White to off-white solid powder
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| LogP |
-2.6
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
785
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| Defined Atom Stereocenter Count |
4
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| SMILES |
P(C([H])([H])P(=O)(O[H])O[H])(=O)(O[H])OC([H])([H])[C@]1([H])[C@]([H])([C@]([H])([C@]([H])(N2C([H])=NC3=C(N=C([H])N=C23)N([H])C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])O1)O[H])O[H]
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| InChi Key |
DMBYYIJBPDWQFF-SCFUHWHPSA-N
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| InChi Code |
InChI=1S/C18H23N5O9P2/c24-14-12(7-31-34(29,30)10-33(26,27)28)32-18(15(14)25)23-9-22-13-16(20-8-21-17(13)23)19-6-11-4-2-1-3-5-11/h1-5,8-9,12,14-15,18,24-25H,6-7,10H2,(H,29,30)(H,19,20,21)(H2,26,27,28)/t12-,14-,15-,18-/m1/s1
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| Chemical Name |
[[(2R,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]methylphosphonic acid
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| Synonyms |
PSB-12379 PSB-12379 disodium N6-Benzyl-α,β-methyleneadenosine 5'-diphosphate disodium salt PSB 12379 PSB12379
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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 |
| 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 : ~125 mg/mL (~242.55 mM)
DMSO : ≥ 5 mg/mL (~9.70 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (194.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9404 mL | 9.7021 mL | 19.4043 mL | |
| 5 mM | 0.3881 mL | 1.9404 mL | 3.8809 mL | |
| 10 mM | 0.1940 mL | 0.9702 mL | 1.9404 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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