8-Br-cADPR
8-Br-cADPR (8-Bromo-Cyclic ADP-Ribose) is a membrane-permeable competitive antagonist of Cyclic ADP-ribose (cADPR) (HY-N7395) and an antagonist of TRPM2 ion channels. 8-Br-cADPR blocks cADPR-dependent RyR, SR calcium mobilization, and cADPR-mediated signaling; reduces Paclitaxel (HY-B0015)-induced axonal calcium flux, and protects against Paclitaxel-induced axonal degeneration/peripheral neuropathy. 8-Br-cADPR blocks isoproterenol-induced pulmonary artery dilation, angiotensin II-induced arterial calcium signaling/contraction, and hypoxic pulmonary vasoconstriction. 8-Br-cADPR can be used in research related to neurological diseases and cancer.
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- CAS. Nr.: 151898-26-9
- Formel: C15H20BrN5O13P2
- Molecular Weight:620.20
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
8‑Br‑cADPR (8-bromo-cADPR) blocks phase 2 HPV in isolated pulmonary artery rings, with a threshold of 3 µM and complete reversal at 100 µM; it blocks isoprenaline (HY-108353)-induced relaxation; and in acutely isolated pulmonary artery smooth muscle cells, it blocks angiotensin II-evoked calcium signaling[4].
8-Br-cADPR does not inhibit the NADase activity of purified human SARM1 in vitro[3].
8-Br-cADPR (100 µM; administered 20 min before and during stimulation) inhibits cADPR and heat-induced OT release in isolated CD38+/+ mouse hypothalamus[1].
8-Br-cADPR partially reduces Paclitaxel (HY-B0015)-induced intra-axonal calcium flux in DRG sensory axons/sensory neuron axons, partially inhibits sTIR dimerization-induced axonal calcium elevation, and reduces Paclitaxel-induced axonal degeneration in a concentration-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
8-Br-cADPR (5-20 nmol; intracerebroventricular injection; single administration; within 10 minutes) attenuates Ropivacaine (HY-B0563)-induced convulsions and reduces hippocampal cADPR, apoptosis, and oxidative stress markers in male Sprague-Dawley rats[2].
8-Br-cADPR (2 mg/kg; intraperitoneal injection; days 4 and 8; two injections total) attenuates Paclitaxel (HY-B0015)-induced mechanical allodynia and partially protects against intraepidermal nerve fiber loss[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 151898-26-9
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Molecular Weight 620.20
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Formel C15H20BrN5O13P2
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C(Br)=NC3=C2N=CN([C@H]4[C@H](O)[C@H](O)[C@@H](COP(O5)(O)=O)O4)C3=N)O[C@@H]1COP5(O)=O
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Synonyms
8-Bromo-Cyclic ADP-Ribose
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Zhong J, et al. Cyclic ADP-Ribose and Heat Regulate Oxytocin Release via CD38 and TRPM2 in the Hypothalamus during Social or Psychological Stress in Mice. Frontiers in neuroscience. 2016;10:304. [Content Brief]
[3]. Li Y, et al. Sarm1 activation produces cADPR to increase intra-axonal Ca++ and promote axon degeneration in PIPN. The Journal of cell biology. 2022 Feb 07;221(2):e202106080. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
8-Br-cADPR Related Classifications
HY-117804 Related Classifications
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