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Dexloxiglumide

Name: Dexloxiglumide
Brand: TargetMol
SKU: T15105
Rating: 4.5 (1 reviews)

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Catalog No. T15105Cas No. 119817-90-2

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. T15105Cas No. 119817-90-2

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$82	5 days	5 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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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

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

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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, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline /PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Stock solution preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(stock solution concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline /PBS/ddH₂O TargetMol | reagent

mix well and clarify

The above example illustrates how to use "In Vivo Formulation Calculator" and does not represent a recommended formulation for any specific compound. Please select an appropriate dissolution method based on your experimental animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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