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Linaclotide

Name: Linaclotide
Brand: TargetMol
SKU: T11852
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11852Cas No. 851199-59-2

Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.

Linaclotide

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Purity: 98.71%

Catalog No. T11852Cas No. 851199-59-2

Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$45	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$197	In Stock	In Stock
25 mg	$347	In Stock	In Stock
50 mg	$516	In Stock	In Stock
100 mg	$736	In Stock	In Stock
200 mg	$987	-	In Stock
1 mL x 10 mM (in DMSO)	$283	In Stock	In Stock

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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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Batch Information

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Purity:98.71%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.
In vitro	Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine, inhibit sodium ion absorption, enhance water secretion into the lumen, and improve defecation; the drug is minimally absorbed into the systemic circulation[2]. In vitro, linaclotide inhibits [125I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner, while binding to membranes from GC-C null mice significantly decreases. Linaclotide is completely degraded after a 30-minute incubation in jejunal fluid in vitro[1].
In vivo	Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation [2]. Pharmacokinetic analysis shows very low oral bioavailability (0.10%). In intestinal secretion and transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: increased fluid secretion into surgically ligated jejunal loops is accompanied by elevated cyclic guanosine-3',5-monophosphate levels and accelerated gastrointestinal transit [1].

Chemical Properties

Molecular Weight	1526.74
Formula	C₅₉H₇₉N₁₅O₂₁S₆
Cas No.	851199-59-2
Smiles	C[C@@H](O)C1NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@H](CSSC[C@H](NC(=O)CNC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(O)=O)NC3=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2
Relative Density.	1.60 g/cm3
Sequence	H-Cys(1)-Cys(2)-Glu-Tyr-Cys(3)-Cys(1)-Asn-Pro-Ala-Cys(2)-Thr-Gly-Cys(3)-Tyr-OH
Sequence Short	CCEYCCNPACTGCY

Storage & Solubility Information

Storage

keep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 20 mg/mL (13.1 mM), Sonication is recommended.

DMSO: 150 mg/mL (98.25 mM)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (1.31 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	0.6550 mL	3.2750 mL	6.5499 mL	32.7495 mL
5 mM	0.1310 mL	0.6550 mL	1.3100 mL	6.5499 mL
10 mM	0.0655 mL	0.3275 mL	0.6550 mL	3.2750 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.0327 mL	0.1637 mL	0.3275 mL	1.6375 mL
50 mM	0.0131 mL	0.0655 mL	0.1310 mL	0.6550 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, 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