Linaclotide

Name: Linaclotide
Brand: MedChemExpress
SKU: HY-17584
Rating: 5.0 (2 reviews)

Cat. No.: HY-17584 Purity: 98.86%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Linaclotide Chemical Structure

CAS No. : 851199-59-2

Size	Price	Stock	Quantity
1 mg	USD 76	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 2 publication(s) in Google Scholar

Other Forms of Linaclotide:

Linaclotide acetate Get quote
Linaclotide (Standard) Get quote

2 Publications Citing Use of MCE Linaclotide

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

In Vitro

Linaclotide inhibits in vitro [¹²⁵I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner. In contrast, [¹²⁵I]-STa binding to these membranes from GC-C null mice is significantly decreased. After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded^[1]. Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine and inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen and improving defecation; the drug is minimally absorbed into the systemic circulation^[2].

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

In Vivo

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: induction of increased fluid secretion into surgically ligated jejunal loops is accompanied by the secretion of elevated levels of cyclic guanosine-3',5-monophosphate and accelerated gastrointestinal transit^[1]. Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation^[2].

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

Clinical Trial

Molecular Weight

1526.74

Formula

C₅₉H₇₉N₁₅O₂₁S₆

CAS No.

851199-59-2

Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (32.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 16.67 mg/mL (10.92 mM; ultrasonic and adjust pH to 2 with HCl)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (1.64 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.64 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (1.64 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 4.17 mg/mL (2.73 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.86%

Select Batch:

Data Sheet (288 KB) SDS (392 KB)

COA (269 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Bryant AP, et al. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci. 2010 May 8;86(19-20):760-5. [Content Brief]

[2]. Love BL, et al. Linaclotide: a novel agent for chronic constipation and irritable bowel syndrome. Am J Health Syst Pharm. 2014 Jul 1;71(13):1081-91. [Content Brief]

Animal Administration
^[1]

Mice: To determine oral bioavailability, three groups (n=3) of female CD-1 mice receive linaclotide (8 mg/kg) intravenously (i.v.), while two groups (n=3) receive linaclotide (8 mg/kg) by gavage (p.o.). Blood is allowed to clot for 5 min, centrifuged at 13,000×g for 3 min, and the serum is collected and stored at −80 °C until sample preparation and analysis by LC-MS/MS^[1].

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

References

[1]. Bryant AP, et al. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci. 2010 May 8;86(19-20):760-5. [Content Brief]

[2]. Love BL, et al. Linaclotide: a novel agent for chronic constipation and irritable bowel syndrome. Am J Health Syst Pharm. 2014 Jul 1;71(13):1081-91. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	0.6550 mL	3.2750 mL	6.5499 mL	16.3748 mL
	5 mM	0.1310 mL	0.6550 mL	1.3100 mL	3.2750 mL
	10 mM	0.0655 mL	0.3275 mL	0.6550 mL	1.6375 mL
DMSO	15 mM	0.0437 mL	0.2183 mL	0.4367 mL	1.0917 mL
	20 mM	0.0327 mL	0.1637 mL	0.3275 mL	0.8187 mL
	25 mM	0.0262 mL	0.1310 mL	0.2620 mL	0.6550 mL
	30 mM	0.0218 mL	0.1092 mL	0.2183 mL	0.5458 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Linaclotide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Linaclotide851199-59-2Guanylate CyclaseInhibitorinhibitorinhibit

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Linaclotide

Customer Review

Other Forms of Linaclotide:

Linaclotide Related Antibodies

2 Publications Citing Use of MCE Linaclotide

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Linaclotide Related Antibodies

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Complete Stock Solution Preparation Table

Linaclotide Related Classifications

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