1. GPCR/G Protein
    Neuronal Signaling
  2. Cholecystokinin Receptor
  3. Pentagastrin

Pentagastrin (Synonyms: ICI-50123)

Cat. No.: HY-A0261 Purity: 99.97%
Handling Instructions

Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury.

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

Pentagastrin Chemical Structure

Pentagastrin Chemical Structure

CAS No. : 5534-95-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 81 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 432 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].

IC50 & Target

IC50: 11 nM (CCKB receptor)[1]

In Vitro

Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca2+ mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca2+ with a maximal increase of 2.77-fold. Binding of 50 pM [125I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260[1].

In Vivo

Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge[2].

Animal Model: Male Sprague-Dawley rats (approximately 200 g)[2]
Dosage: 80 µg/kg/h
Administration: Intravenous injection
Result: Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.
Molecular Weight

767.89

Formula

C₃₇H₄₉N₇O₉S

CAS No.

5534-95-2

SMILES

O=C(N[[email protected]@H](CCSC)C(N[[email protected]@H](CC(O)=O)C(N[[email protected]](C(N)=O)CC1=CC=CC=C1)=O)=O)[[email protected]@H](NC(CCNC(OC(C)(C)C)=O)=O)CC2=CNC3=C2C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (44.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3023 mL 6.5113 mL 13.0227 mL
5 mM 0.2605 mL 1.3023 mL 2.6045 mL
10 mM 0.1302 mL 0.6511 mL 1.3023 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Pentagastrin
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