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Dexloxiglumide

Name: Dexloxiglumide
Brand: TargetMol
SKU: T15105
Price: 82 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T15105 Copy Product Info

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Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist and the pharmacologically active enantiomer of Loxiglumide, effectively inhibiting smooth muscle contractions induced by cholecystokinin-octapeptide (CCK-8), while displaying moderate, polarized, concentration-dependent, and pH-dependent Caco-2 permeability and increasing uptake of the MRP1 substrate fluorescein. Dexloxiglumide supports the mechanistic studies of gastrointestinal disorders and tumor-related smooth muscle and transporter biology.

Dexloxiglumide

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Catalog No. T15105

Cas No. 119817-90-2

Pack Size	Price	USA Stock	Global Stock	Quantity
2 mg	$82	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist and the pharmacologically active enantiomer of Loxiglumide, effectively inhibiting smooth muscle contractions induced by cholecystokinin-octapeptide (CCK-8), while displaying moderate, polarized, concentration-dependent, and pH-dependent Caco-2 permeability and increasing uptake of the MRP1 substrate fluorescein. Dexloxiglumide supports the mechanistic studies of gastrointestinal disorders and tumor-related smooth muscle and transporter biology.
In vitro	In ex vivo studies utilizing human isolated gallbladder, Dexloxiglumide stimulated P-gp ATPase activity at concentrations > 17.3 μM, increased fluorescein uptake by 4-fold at 433 μM indicating MRP1 inhibition [1].
In vivo	In rat models, intravenous administration of Dexloxiglumide dose-dependently inhibited the delay in gastric emptying induced by CCK-8, with an ID50 of 1.14 mg/kg. The compound demonstrated selectivity for the CCK1 receptor, as it did not affect pentagastrin-induced acid secretion, a process mediated by CCK2 (CCK-B) receptors, even at doses that fully blocked CCK1-mediated motility effects [1].

Chemical Properties

Molecular Weight	461.38
Formula	C₂₁H₃₀Cl₂N₂O₅
Cas No.	119817-90-2
Smiles	[C@@H](C(N(CCCCC)CCCOC)=O)(NC(=O)C1=CC(Cl)=C(Cl)C=C1)CCC(O)=O
Relative Density.	1.233 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (86.7 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (5.42 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1674 mL	10.8371 mL	21.6741 mL	108.3705 mL
5 mM	0.4335 mL	2.1674 mL	4.3348 mL	21.6741 mL
10 mM	0.2167 mL	1.0837 mL	2.1674 mL	10.8371 mL
20 mM	0.1084 mL	0.5419 mL	1.0837 mL	5.4185 mL
50 mM	0.0433 mL	0.2167 mL	0.4335 mL	2.1674 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc