2′-Deoxy-ADPR
2′-Deoxy-ADPR is an endogenous TRPM2 agonist that activates Ca2+-permeable cation channels. 2′-Deoxy-ADPR activates the Ca2+ sensitivity of TRPM2, increasing whole-cell currents by slowing inactivation and increasing open probability. 2′-Deoxy-ADPR can be used in research related to TRPM2 channel-mediated diseases, such as inflammation and immune-related diseases.
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- CAS No.: 111864-49-4
- Formule: C15H23N5O13P2
- Masse moléculaire:543.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
TRPM2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
192 nM
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Activation of human TRPM2 in HEK293 cells stably expressing hsTRPM2 by 2′-Deoxy-ADPR assessed via whole-cell patch clamp with 100 μM intracellular 2dADPR and voltage ramps from -85 mV to +20 mV every 5 s over 445 s.
Activation of human TRPM2 in HEK293 cells stably expressing hsTRPM2 by 2′-Deoxy-ADPR assessed via whole-cell patch clamp with 100 μM intracellular 2dADPR and voltage ramps from -85 mV to +20 mV every 5 s over 445 s.
|
38318185 |
In Vitro
2′-deoxy-ADPR is generated by hydrolysis of 2′-deoxy-NAD by recombinant human CD38[1].
2′-deoxy-ADPR is a highly potent TRPM2 agonist in HEK293 cells expressing hTRPM2, producing whole-cell currents 10.4-fold higher than ADPR, with maximal currents of 14.3-16.7 nA under 50-200 nM free Ca2+ conditions[1].
2′-deoxy-ADPR increases the open probability to a median of 0.92 in excised inside-out membrane patches from HEK293 cells expressing hTRPM2, and slows inactivation, but does not alter single-channel conductance[1].
2′-deoxy-ADPR is endogenously present in Jurkat T cells at 35 pmol per 107 cells (approximately 9.8 µM in the cytosol), and H2O2 increases it 2.71-fold to 95 pmol per 107 cells[1].
2′-Deoxy-ADPR (2dADPR) (100 μM) activates hsTRPM2 in HEK293 cells with an EC50 of 192 nM; at intracellular Ca2+ concentrations below 1 μM, it activates the channel faster than ADPR in HEK293 cells expressing hsTRPM2[2].
In transfected HEK293 cells, the W1355A mutation in the NUDT9H domain of 2′-Deoxy-ADPR eliminates the difference in activation rate between it and ADPR[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 111864-49-4
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Masse moléculaire 543.32
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Formule C15H23N5O13P2
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SMILES
O[C@H]1C[C@H](N(C=N2)C3=C2C(N)=NC=N3)O[C@@H]1COP(OP(OC[C@@H]4[C@@H](O)[C@@H](O)C(O)O4)(O)=O)(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)