2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. SR 146131

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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 671 In-stock
Solution
10 mM * 1 mL in DMSO USD 671 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1850 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

SR 146131 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

SR 146131 Related Antibodies
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].

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

610.16

Formula

C32H36ClN3O5S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (409.73 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 1.6389 mL 8.1946 mL 16.3891 mL
5 mM 0.3278 mL 1.6389 mL 3.2778 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6389 mL 8.1946 mL 16.3891 mL 40.9729 mL
5 mM 0.3278 mL 1.6389 mL 3.2778 mL 8.1946 mL
10 mM 0.1639 mL 0.8195 mL 1.6389 mL 4.0973 mL
15 mM 0.1093 mL 0.5463 mL 1.0926 mL 2.7315 mL
20 mM 0.0819 mL 0.4097 mL 0.8195 mL 2.0486 mL
25 mM 0.0656 mL 0.3278 mL 0.6556 mL 1.6389 mL
30 mM 0.0546 mL 0.2732 mL 0.5463 mL 1.3658 mL
40 mM 0.0410 mL 0.2049 mL 0.4097 mL 1.0243 mL
50 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8195 mL
60 mM 0.0273 mL 0.1366 mL 0.2732 mL 0.6829 mL
80 mM 0.0205 mL 0.1024 mL 0.2049 mL 0.5122 mL
100 mM 0.0164 mL 0.0819 mL 0.1639 mL 0.4097 mL
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SR 146131 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:

SR 146131221671-61-0SR146131SR-146131Cholecystokinin ReceptorCCK ReceptorInhibitorinhibitorinhibit

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