1. GPCR/G Protein
  2. Guanylate Cyclase
  3. Plecanatide

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

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Plecanatide Chemical Structure

Plecanatide Chemical Structure

CAS No. : 467426-54-6

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5 mg USD 230 In-stock
10 mg USD 380 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis[1][2][3].

IC50 & Target

EC50: 190 nM (guanylate cyclase-C)[1]

In Vitro

Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cyclic guanosine monophosphate (cGMP) synthesis in a dose-dependent manner with EC50 of 190 nM in T84 cells[1].

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

In Vivo

Plecanatide (0.5 and 2.5 mg/kg, p.o.) ameliorates spontaneous and chemically induced colitis after treatment for 7 days in BALB/c mice, and 14 days in TCRα-/- mice[1].
Plecanatide (0.005-5 mg/kg, once daily for 7 days) also shows anti-inflammatory activity in dextran sulfate sodium (DSS) and trinitrobenzene sulfonic (TNBS)-induced colitis in BDF-1 mice[1].

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

Animal Model: Female BALB/c mice (2-4 month old) are induced colitis by TNBS[1]
Dosage: 0, 0.5 and 2.5 mg/kg
Administration: P.o. for 7 days
Result: Effectively reduced colitis severity scores as compared to vehicle treatment.
Clinical Trial
Molecular Weight

1681.89

Formula

C65H104N18O26S4

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)

Sequence Shortening

NDECELCVNVACTGCL (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)

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 : 100 mg/mL (59.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5946 mL 2.9728 mL 5.9457 mL
5 mM 0.1189 mL 0.5946 mL 1.1891 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.5946 mL 2.9728 mL 5.9457 mL 14.8642 mL
5 mM 0.1189 mL 0.5946 mL 1.1891 mL 2.9728 mL
10 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4864 mL
15 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9909 mL
20 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
25 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 mL
30 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4955 mL
40 mM 0.0149 mL 0.0743 mL 0.1486 mL 0.3716 mL
50 mM 0.0119 mL 0.0595 mL 0.1189 mL 0.2973 mL
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Plecanatide 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.

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Product Name:
Plecanatide
Cat. No.:
HY-108741
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