1. GPCR/G Protein
  2. Cholecystokinin Receptor

SR 146131 

Cat. No.: HY-11077
Handling Instructions

SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

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

SR 146131 Chemical Structure

SR 146131 Chemical Structure

CAS No. : 221671-61-0

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

IC50 & Target

Cholecystokinin 1 receptor[1]

In Vitro

SR 146131 inhibits in the binding of [125I]-BH-CCK-8S to CCK1sites on 3T3-hCCK1 cell membranes with an IC50 value of 0.56 ± 0.10 nM. At much higher concentrations, SR 146131 also inhibits the binding of radiolabeled CCK to CCK2sites in CHO-hCCK2 membranes with an IC50 of 162 ± 27 nM. SR 146131 is a potent CCK1 agonist on several intracellular events linked to CCK1 receptor activation in various cell types: on [Ca2+]i release and IP1 formation, SR 146131 appears as a full CCK1 receptor agonist in the 3T3-hCCK1 cells, but a partial CCK1receptor agonist on MAPK activation and early gene expression in this cell line. SR 146131 also acts as a partial agonist in the two neuroblastoma cell lines[1].

In Vivo

SR 146131 completely inhibits gastric and gallbladder emptying in mice (ED50 of 66 and 2.7 μg/kg p.o., respectively). SR 146131 dose dependently reduces food intake in fasted rats (from 0.1 mg/kg p.o.), in nonfasted rats in which food intake has been highly stimulated by the administration of neuropeptide Y (1–36) (from 0.3 mg/kg p.o.), in fasted gerbils (from 0.1 mg/kg p.o.), and in marmosets maintained on a restricted diet (from 3 mg/kg p.o.). SR 146131 (10 mg/kg p.o.) also increases the number of Fos-positive cells in the hypothalamic paraventricular nucleus of rats. Locomotor activity of mice is reduced by orally administered SR 146131 (from 0.3 mg/kg p.o.)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6389 mL 8.1946 mL 16.3891 mL
5 mM 0.3278 mL 1.6389 mL 3.2778 mL
10 mM 0.1639 mL 0.8195 mL 1.6389 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

3T3-hCCK1 cells grown to subconfluence in 6-well cluster plates are washed with fresh medium. Twenty-four hours later, the cells are stimulated for 15 min with various concentrations of CCK-8S or SR 146131[1].

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

Animal Administration
[1]

Rats[1]

Male Sprague-Dawley rats are fasted for 18 h, and allowed access to food for only 6 h between 10 AM and 4 PM each day. Water is available ad libitum. At the end of this adaptation phase, rats are administered SR 146131 (0.03-3 mg/kg p.o.). One hour after SR 146131 administration, a weighed amount of food is introduced into the cage, and food intake is measured 1, 3, 6, and 23 h after SR 146131 administration[1].

Mice[1]

SR 146131 (0.01-1 pg) is solubilized in DMSO (1 mg/mL), diluted to the required concentrations with water, and injected (in 1 μL) into one striatum in awake, hand-restrained female CD1 mice (25-30 g). After injection, the animals are placed individually in Plexiglas cages (10 × 10 × 15 cm). Turning behavior in mice is monitored[1].

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

References
Molecular Weight

610.16

Formula

C₃₂H₃₆ClN₃O₅S

CAS No.

221671-61-0

SMILES

O=C(O)CN1C(C(NC2=NC(C3=CC(OC)=C(Cl)C=C3OC)=C(CCC4CCCCC4)S2)=O)=CC5=C1C(C)=CC(C)=C5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SR 146131
Cat. No.:
HY-11077
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SR 146131

Cat. No.: HY-11077