Art. -Nr.: HY-B1451A

Imidapril

(Synonyms: TA-6366 free base)

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Imidapril (TA-6366 free base) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions.

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Reinheit: 99.0%
CAS. Nr.: 89371-37-9
Formel: C₂₀H₂₇N₃O₆
Molecular Weight:405.44

Speicherung:

-20°C, protect from light

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

Imidapril Chemical Structure

CAS. Nr.: 89371-37-9

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

MMP-9

Alle MMP Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

In Vitro

Imidapril (1×10^-9-1×10^-7 μM; 2 h pre-treatment followed by 1 h LPS stimulation) inhibits the activation of the MKK4-JNK-c-Jun signaling pathway in LPS-induced human primary monocytes, with no effect on the activation of p38, ERK, or NF-κB p65^[1].
Imidapril (0.1 μM; pre-treatment for 2 h followed by stimulation with LPS or poly I:C for 24 h) significantly downregulates LPS-induced TNF-α production and poly I:C-induced IP-10 production in THP-1 cells^[1].
Imidapril (10^-7-10^-4 M) dose-dependently inhibits the gelatinase activity of recombinant MMP-9 in a cell-free in vitro system^[3].

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

In Vivo

Imidapril (1-5 mg/kg/day; p.o.; ad libitum in drinking water; daily; 12 weeks) prevents the progression of diabetic nephropathy in db/db mice in a dose-dependent manner, reducing systolic blood pressure (at 5 mg/kg/day), mesangial expansion, urinary albumin excretion, urinary 8-OHdG levels, and glomerular 8-OHdG-positive cell counts, without affecting blood glucose or body weight^[2].
Imidapril (3 mg/kg/day; i.p.; continuous; 1 month) suppresses cerebral aneurysm formation and medial thinning in rats via an ACE-independent, MMP-9-dependent mechanism, reducing mean aneurysm size to 32.9 mm and increasing mean medial thickness ratio to 0.73 without altering blood pressure^[3].

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

Chemical Information

CAS. Nr. 89371-37-9
Appearance Solid
Molecular Weight 405.44
Formel C₂₀H₂₇N₃O₆
Color White to off-white
SMILES

O=C(N(C1=O)[C@@H](CN1C)C(O)=O)[C@H](C)N[C@H](C(OCC)=O)CCC2=CC=CC=C2
Synonyms

TA-6366 free base
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (123.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.4665 mL

12.3323 mL

24.6646 mL

5 mM

0.4933 mL

2.4665 mL

4.9329 mL

10 mM

0.2466 mL

1.2332 mL

2.4665 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: ≥ 1.25 mg/mL (3.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (278 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)
- 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]. Tsai MK, et al. Suppressive effects of imidapril on Th1- and Th2-related chemokines in monocytes. J Investig Med. 2011;59(7):1141-1146. [Content Brief]

[2]. Naito Y, et al. Imidapril, an angiotensin-converting enzyme inhibitor, reduces diabetes-induced renal oxidative damage in mice[J]. Journal of Clinical Biochemistry and Nutrition, 2005, 37(1): 29-37.

[3]. Ishibashi R, et al. Imidapril inhibits cerebral aneurysm formation in an angiotensin-converting enzyme-independent and matrix metalloproteinase-9-dependent manner. Neurosurgery. 2012;70(3):722-730. [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	2.4665 mL	12.3323 mL	24.6646 mL	61.6614 mL
	5 mM	0.4933 mL	2.4665 mL	4.9329 mL	12.3323 mL
	10 mM	0.2466 mL	1.2332 mL	2.4665 mL	6.1661 mL
	15 mM	0.1644 mL	0.8222 mL	1.6443 mL	4.1108 mL
	20 mM	0.1233 mL	0.6166 mL	1.2332 mL	3.0831 mL
	25 mM	0.0987 mL	0.4933 mL	0.9866 mL	2.4665 mL
	30 mM	0.0822 mL	0.4111 mL	0.8222 mL	2.0554 mL
	40 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5415 mL
	50 mM	0.0493 mL	0.2466 mL	0.4933 mL	1.2332 mL
	60 mM	0.0411 mL	0.2055 mL	0.4111 mL	1.0277 mL
	80 mM	0.0308 mL	0.1542 mL	0.3083 mL	0.7708 mL
	100 mM	0.0247 mL	0.1233 mL	0.2466 mL	0.6166 mL

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Imidapril

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Alle MMP Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Imidapril Related Classifications

Art. -Nr.: HY-B1451A