Art. -Nr.: HY-121872

DP-b99

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DP-b99 is a blood-brain barrier-permeable inhibitor of CYP2C9 and MMP-9, with a K_i 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 95.0%
CAS. Nr.: 222315-88-0
Formel: C₄₂H₆₄N₂O₁₂
Molecular Weight:788.96

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DP-b99 Chemical Structure

CAS. Nr.: 222315-88-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

MMP9	CYP2C9 4.655 μM (Ki)

Alle MMP Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

In Vitro

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.

In Vivo

DP-b99 (0.3 mg/kg; intraperitoneal injection; once daily for 9 consecutive days) significantly delays pentylenetetrazol (PTZ)-induced seizures in C57Bl/6 mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57Bl/6 (male, 3 months old, 25-30 g, PTZ-induced kindling model)^[2]
Dosage:

0.3 mg/kg/day
Administration:

i.p.; once daily; 3 hours prior to PTZ injection for 9 days
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 222315-88-0
Appearance Solid
Molecular Weight 788.96
Formel C₄₂H₆₄N₂O₁₂
Color White to light yellow
SMILES

O=C(CN(C1=CC=CC=C1OCCOC2=CC=CC=C2N(CC(OCCOCCCCCCCC)=O)CC(O)=O)CC(O)=O)OCCOCCCCCCCC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2675 mL

6.3375 mL

12.6749 mL

5 mM

0.2535 mL

1.2675 mL

2.5350 mL

10 mM

0.1267 mL

0.6337 mL

1.2675 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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DP-b99

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

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Anti-Rheumatic Arthritis Compound Library

Alle MMP Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DP-b99 Related Classifications

HY-121872 Related Classifications