8-Br-ADPR disodium
Based on 1 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C15H20BrN5Na2O14P2
- 분자량:682.18
-
보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocol
- 순도&문서
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) 8-Br-ADPR disodium
More
Biological Activity
제품 설명
|
CaMK II |
In Vitro
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.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
Result:Blocked the B16F10-induced translocation of perforin and granzyme B towards the immunological synapse between NK cells and B16F10 cells.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
Result:Inhibited the PME-induced translocation of perforin and granzyme B from intracellular granules to plasma membrane-enriched fractions.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
Result:Inhibited B16F10-induced granzyme B secretion from NK cells, reducing the amount of granzyme B released into the culture medium.
In Vivo
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.
-
Animal Model:C57BL/6J mice with Physiological fasting (male, 8-12 weeks old)[1]
-
Dosage:32 mg/kg
-
Administration:i.v.; single dose
-
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.
-
Animal Model:B6.BKS(D)-Leprdb/J mice with Diabetes (db/db) (male, 8-12 weeks old)[1]
-
Dosage:32 mg/kg
-
Administration:i.v.; single dose
-
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
-
Appearance Solid
-
분자량 682.18
-
화학식 C15H20BrN5Na2O14P2
-
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
-
Synonyms
8-Bromoadenosine-5'-O-diphosphoribose disodium
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
-
Journal Impact Factor
-
Most Recent
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
8-Br-ADPR disodium Related Classifications
HY-134261A Related Classifications
Powered by Bioz