8-Br-ADPR disodium
Based on 1 Customer Validation
8-Br-ADPR disodium (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR disodium inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR disodium significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR disodium effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR disodium is widely used in studies related to diseases such as diabetes, melanoma and lymphoma.
For research use only. We do not sell to patients.
- Formula: C15H20BrN5Na2O14P2
- Molecular Weight:682.18
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CaMK II |
8-Br-ADPR (100 μM; preincubated prior to glucagon treatment) disodium specifically blocks glucagon-induced sustained nuclear calcium signals in mouse primary hepatocytes, without altering cytosolic calcium signals[1].
8-Br-ADPR (100 μM; 30 min preincubated before ADPR treatment) disodium completely blocks ADPR-induced calcium flux between the perinuclear space and nucleoplasm in isolated nuclei from mouse primary hepatocytes[1].
8-Br-ADPR (100 μM; 30 min preincubated before 100 nM glucagon treatment for 4 h) disodium significantly reduces glucagon-induced G6pc and Pck1 mRNA expression in mouse primary hepatocytes[1].
8-Br-ADPR (100 μM; 20 min) disodium inhibits B16F10-induced translocation of perforin and granzyme B to the immunological synapse in murine NK cells[2].
8-Br-ADPR (100 μM; 20 min) disodium reduces the cytolytic activity of murine NK cells against B16F10 melanoma target cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Blocked the B16F10-induced translocation of perforin and granzyme B towards the immunological synapse between NK cells and B16F10 cells.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Inhibited the PME-induced translocation of perforin and granzyme B from intracellular granules to plasma membrane-enriched fractions.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Inhibited B16F10-induced granzyme B secretion from NK cells, reducing the amount of granzyme B released into the culture medium.
8-Br-ADPR (32 mg/kg; i.v.; single dose) disodium reduces pyruvate-induced blood glucose levels in diabetic db/db mice by inhibiting hepatic gluconeogenic gene expression and CRE-mediated transcriptional activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with Physiological fasting (male, 8-12 weeks old)[1]
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Dosage:32 mg/kg
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Administration:i.v.; single dose
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Result:Reduced hepatic CRE luciferase activity.
Lowered liver G6pc and Pck1 mRNA levels by ~50% each.
Decreased pyruvate tolerance test blood glucose levels by ~30-40% across 0-90 minutes post-pyruvate injection.
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Animal Model:B6.BKS(D)-Leprdb/J mice with Diabetes (db/db) (male, 8-12 weeks old)[1]
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Dosage:32 mg/kg
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Administration:i.v.; single dose
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Result:Reduced hepatic CRE luciferase activity.
Decreased liver G6pc mRNA levels by ~40% and Pck1 mRNA levels by ~30%.
Reduced pyruvate tolerance test blood glucose levels by ~60-70% across all time points.
Chemical Information
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Appearance Solid
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Molecular Weight 682.18
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Formula C15H20BrN5Na2O14P2
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C(Br)=NC3=C2N=CN=C3N)O[C@@H]1COP(OP(OC[C@H]4OC(O)[C@H](O)[C@@H]4O)(O[Na])=O)(O[Na])=O
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Synonyms
8-Bromoadenosine-5'-O-diphosphoribose disodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
8-Br-ADPR disodium Related Classifications
HY-134261A Related Classifications
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