5-BDBD |
Katalog-Nr.GC13943
One-Click Copy Product Info
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5-BDBD, ein potenter und selektiver P2X4-Rezeptorantagonist, hemmt rP2X4R-vermittelte StrÖme mit einem IC50 von 0,75 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 768404-03-1
Sample solution is provided at 25 µL, 10mM.
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5-BDBD is a potent and selective P2X4 receptor antagonist with an IC50 value of 0.5-0.75µM, capable of inhibiting rP2X4R-mediated currents[1-2]. 5-BDBD can alleviate asthma symptoms and has potential for treating alcoholic fatty liver disease[3-4].
In vitro, treatment of prostate cancer cells (DU145 cells) with 5-BDBD (5 or 10µM) for 24 to 72 hours significantly inhibited their migration and invasion capabilities and induced the expression of the apoptosis marker cleaved caspase-3[5]. Treatment of primary rat osteoblasts with 5-BDBD (0.1-10µM) for 14 days dose-dependently inhibited bone nodule formation and reduced alkaline phosphatase activity[6].
In vivo, continuous administration of 5-BDBD (1.0mM; via an implanted osmotic pump at a flow rate of 1.0µL/h for 3 days) to adult male Sprague-Dawley rats subjected to cortical contusion injury (CCI) significantly suppressed the activation of microglia in the ipsilateral cortex and hippocampus and reduced Iba-1 protein expression levels. 5-BDBD also significantly decreased the levels of pro-inflammatory cytokines in the ipsilateral cortex and hippocampus[7]. Treatment of 8-12-week-old wild-type mice subjected to 60 minutes of middle cerebral artery occlusion (MCAo) with 5-BDBD (1mg/kg; administered orally daily for 3 days) significantly reduced infarct volume and neurological deficit scores at 3 days after stroke, and decreased the levels of the pro-inflammatory cytokine IL-1β and blood-brain barrier permeability[8].
References:
[1] Long T, He W, Pan Q, et al. Microglia P2X4 receptor contributes to central sensitization following recurrent nitroglycerin stimulation. J Neuroinflammation. 2018 Aug 30;15(1):245.
[2] Coddou C, Sandoval R, Hevia MJ, et al. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett. 2019 Jan 18;690:219-224.
[3] Hu B, Feng X, Wang L, et al. 5-BDBD ameliorates an OVA-induced allergic asthma by the reduction of Th2 cytokines production. Iran J Basic Med Sci. 2018 Apr;21(4):364-369.
[4] Xia GQ, Cai JN, Wu X, et al. The mechanism by which ATP regulates alcoholic steatohepatitis through P2X4 and CD39. Eur J Pharmacol. 2022 Feb 5;916:174729.
[5] Maynard JP, Lu J, Vidal I, et al. P2X4 purinergic receptors offer a therapeutic target for aggressive prostate cancer. J Pathol. 2022 Feb;256(2):149-163.
[6] Orriss IR, Davies BK, Bourne LE, et al. Modulation of osteoblast differentiation and function by the P2X4 receptor. Purinergic Signal. 2023 Jun;19(2):367-378.
[7] Kobayashi M, Moro N, Yoshino A, et al. Inhibition of P2X4 and P2X7 receptors improves histological and behavioral outcomes after experimental traumatic brain injury in rats. Exp Ther Med. 2023 Jun 23;26(2):378.
[8] Srivastava P, Cronin CG, Scranton VL, et al. Neuroprotective and neuro-rehabilitative effects of acute purinergic receptor P2X4 (P2X4R) blockade after ischemic stroke. Exp Neurol. 2020 Jul;329:113308.
| Cell experiment [1]: | |
Cell lines | DU145 cells (human prostate cancer cell line) |
Preparation Method | DU145 cells were maintained in MEM supplemented with 10% fetal bovine serum (FBS). Cells were treated with 5-BDBD at concentrations of 5 or 10µM for 24-72 hours. |
Reaction Conditions | 5 or 10µM; 24-72 hours. |
Applications | 5-BDBD treatment significantly decreased DU145 cell viability and migration. |
| Animal experiment [2]: | |
Animal models | 8-12-week-old male and female wild-type C57B/6 mice. |
Preparation Method | Mice were subjected to a 60-minute right middle cerebral artery occlusion (MCAo) followed by reperfusion. The P2X4R antagonist 5-BDBD (1mg/kg) or vehicle (0.5% methyl cellulose) was administered orally (P.O.) daily for 3 days, starting 4 hours after MCAo. |
Dosage form | 1mg/kg; P.O.; Daily for 3 days. |
Applications | 5-BDBD treatment significantly reduced infarct volume and neurological deficit (ND) score at 3 days after stroke. 5-BDBD also significantly reduced mortality by day 30 after stroke. |
References: | |
| Cas No. | 768404-03-1 | SDF | |
| Chemical Name | 5-(3-bromophenyl)-1H-benzofuro[3,2-e][1,4]diazepin-2(3H)-one | ||
| Canonical SMILES | BrC1=CC(C2=NCC(NC3=C2OC4=CC=CC=C34)=O)=CC=C1 | ||
| Formula | C17H11BrN2O2 | M.Wt | 355.19 |
| Löslichkeit | <35.52mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8154 mL | 14.077 mL | 28.1539 mL |
| 5 mM | 563.1 μL | 2.8154 mL | 5.6308 mL |
| 10 mM | 281.5 μL | 1.4077 mL | 2.8154 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)