Linaclotide

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

Cat. No.: HY-17584 Pureza: 99.77%: Ficha de datos
COA

SDS
Instrucciones de manejo
FAQs
Technical Support

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Síntesis de péptidos personalizados

Linaclotide Estructura química

No. CAS : 851199-59-2

Tamaño	Stock	Cantidad
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

or Consulta para venta a granel

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of Linaclotide:

Linaclotide acetate In-stock
Linaclotide-d₄ Obtener un presupuesto
Linaclotide (Standard) Obtener un presupuesto

2 Publications Citing Use of MCE Linaclotide

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica
Protocolo
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

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.

Ensayo clínico

Peso molecular

1526.74

Fòrmula

C₅₉H₇₉N₁₅O₂₁S₆

No. CAS

851199-59-2

Appearance

Solid

Color

White to off-white

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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)

Solvente y solubilidad

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.

Calculadora de molaridad
Calculadora de dilución

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).

Pureza y Documentación

Purity: 99.77%

Select Batch:

Ficha de datos (288 KB) SDS (392 KB)

COA (269 KB) RP-HPLC (264 KB) MS (68 KB) Elemental Analysis Report (127 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Administraciòn de animales
^[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

Referencias

[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

Productos vistos recientemente:

Nombre del producto

Requested Quantity *

Nombre del solicitante *

Saludo

Direcciòn del E-mail *

Número de teléfono *

Department

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

Observaciones

Nombre del producto

Lot #

Nombre del solicitante *

Direcciòn del E-mail *

Número de teléfono

Department *

Nombre de la Organizaciòn *

Country or Region *

Observaciones

Name
E-mail *

	Sorry, but the email address you supplied was invalid.

Linaclotide

Revisión del cliente

Other Forms of Linaclotide:

Linaclotide Related Antibodies

2 Publications Citing Use of MCE Linaclotide

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Protocolo

Pureza y Documentación

Referencias

Revisión del cliente

Linaclotide Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Linaclotide Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report