DP-b99
Based on 1 Customer Validation
DP-b99 is a blood-brain barrier-permeable inhibitor of CYP2C9 and MMP-9, with a Ki value of 4.655 μM against CYP2C9. DP-b99 inhibits CYP2C9 via apparent non-competitive inhibition, mainly chelates pathological Zn2+ in the membrane environment, attenuates the elevation of intracellular Zn2+ and Ca2+ levels, delays seizure onset and reduces seizure severity, and also prevents MMP-9-dependent dendritic spine remodeling, β-dystroglycan cleavage and gelatinase activity. DP-b99 can be used in the research of acute ischemic stroke, epileptogenesis and stroke.
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- Pureza: 95.0%
- No. CAS: 222315-88-0
- Fòrmula: C42H64N2O12
- Peso molecular:788.96
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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MMP9 |
CYP2C9 4.655 μM (Ki) |
DP-b99 (0.12-20 μM; 25 h) significantly reduces neuronal death in rat organotypic hippocampal slice cultures induced by Kainic acid (HY-N2309)[2].
DP-b99 (0.12-20 μM; 1 h 10 min) inhibits KA-induced cleavage of β-dystroglycan, a marker of MMP-9 activity, in rat organotypic hippocampal slice cultures[2].
DP-b99 (0.12-20 μM; 2 h) inhibits MMP-9-induced dendritic spine elongation and F-actin redistribution in primary cultured rat hippocampal neurons[2].
DP-b99 (20 μM) is a cell-permeable chelator that reduces elevated intracellular Zn2+ in MIN6 mouse insulinoma cells to resting levels, even in the presence of physiological extracellular Ca2+[3].
DP-b99 (0.01-20 μM; 20-30 min) dose-dependently attenuates L-type Ca2+ channel-mediated Zn2+ influx in MIN6 mouse insulinoma cells[3].
DP-b99 (20 μM; 1 h) reduces the rate and amplitude of Zn2+ influx through L-type Ca2+ channels by 4-fold in primary rat embryonic cortical neurons[3].
DP-b99 (20 μM; 1 h) reduces the elevation amplitude of intracellular Ca2+ in primary rat embryonic cortical neurons by 6-fold via L-type Ca2+ channels[3].
DP-b99 (20 μM; 1 h) reduces depolarization-induced Zn2+ influx in the hippocampal pyramidal cell layer of acute mouse brain slices by approximately 6-fold[3].
DP-b99 (20 μM) reduces the rate and amplitude of Zn2+ influx induced by the ionophore Pyrithione (HY-B1747) in primary rat embryonic cortical neurons by 2-fold, indicating that its activity is independent of ion entry pathways[3].
DP-b99 (20 μM; 1 h) reduces Zn2+ -induced neuronal mortality from 30% to 17% in primary rat embryonic cortical neurons via L-type Ca2+ channels[3].
DP-b99 (20 μM; 1 h) reduces the mortality rate of primary rat embryonic cortical neurons induced by Zn2+/Pyrithione from approximately 45%-52% to 30%, indicating that it exhibits protective activity independent of the Zn2+ entry pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (male, 3 months old, 25-30 g, PTZ-induced kindling model)[2]
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Dosage:0.3 mg/kg/day
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Administration:i.p.; once daily; 3 hours prior to PTZ injection for 9 days
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Result:Significantly delayed the development of PTZ-induced kindled seizures.
Significantly reduced mossy fiber sprouting in the CA3 hippocampal area.
Diminished the cleavage of β-dystroglycan (β-DG) to its 30 kDa form, a marker of MMP-9 activity, compared to vehicle-treated kindled mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 222315-88-0
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Appearance Solid
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Peso molecular 788.96
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Fòrmula C42H64N2O12
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Color White to light yellow
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SMILES
O=C(CN(C1=CC=CC=C1OCCOC2=CC=CC=C2N(CC(OCCOCCCCCCCC)=O)CC(O)=O)CC(O)=O)OCCOCCCCCCCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (126.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.17 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1].
Rosenberg G, et al. The neuroprotective agent DP-b99 does not interact with s-warfarin in vivo despite significant CYP2C9 inhibition in vitro. Basic Clin Pharmacol Toxicol. 2011 Apr;108(4):289-92.
[Content Brief]
[2].
Yeghiazaryan M, et al. DP-b99 modulates matrix metalloproteinase activity and neuronal plasticity. PLoS One. 2014 Jun 11;9(6):e99789.
[Content Brief]
[3].
Barkalifa R, et al. The lipophilic zinc chelator DP-b99 prevents zinc induced neuronal death. Eur J Pharmacol. 2009 Sep 15;618(1-3):15-21.
[Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2675 mL | 6.3375 mL | 12.6749 mL | 31.6873 mL |
| 5 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3375 mL | |
| 10 mM | 0.1267 mL | 0.6337 mL | 1.2675 mL | 3.1687 mL | |
| 15 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL | |
| 20 mM | 0.0634 mL | 0.3169 mL | 0.6337 mL | 1.5844 mL | |
| 25 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL | |
| 30 mM | 0.0422 mL | 0.2112 mL | 0.4225 mL | 1.0562 mL | |
| 40 mM | 0.0317 mL | 0.1584 mL | 0.3169 mL | 0.7922 mL | |
| 50 mM | 0.0253 mL | 0.1267 mL | 0.2535 mL | 0.6337 mL | |
| 60 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5281 mL | |
| 80 mM | 0.0158 mL | 0.0792 mL | 0.1584 mL | 0.3961 mL | |
| 100 mM | 0.0127 mL | 0.0634 mL | 0.1267 mL | 0.3169 mL |
DP-b99 Related Classifications
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