2. GPCR/G Protein
  3. Motilin Receptor
  4. Camicinal

Camicinal  (Synonyms: GSK962040)

Cat. No.: HY-10922 Purity: 95.94%
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Camicinal (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.

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

Camicinal Chemical Structure

Camicinal Chemical Structure

CAS No. : 923565-21-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Camicinal:

Camicinal Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Camicinal

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Camicinal (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.

IC50 & Target

pEC50: 7.9 (Motilin Receptor)[1].
In Vitro

Camicinal (GSK962040) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal (GSK962040) 300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and Camicinal (GSK962040) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) [1]. Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. Camicinal (GSK962040) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM [3].

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

Camicinal Related Antibodies
In Vivo

Camicinal (GSK962040) (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g; P < 0.05) [1]. Camicinal (GSK962040) induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >1.14 μmol L 1. After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned. Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) [2]. he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%. Camicinal (GSK962040) shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) [3]. Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only [4].

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

424.55

Formula

C25H33FN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC(NC2=CC=CC(F)=C2)CC1)CC3=CC=C(CN4C[C@H](C)NCC4)C=C3
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 : 100 mg/mL (235.54 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 2.3554 mL 11.7772 mL 23.5544 mL
5 mM 0.4711 mL 2.3554 mL 4.7109 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.

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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: ≥ 2.5 mg/mL (5.89 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 (5.89 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.
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

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 2.3554 mL 11.7772 mL 23.5544 mL 58.8859 mL
5 mM 0.4711 mL 2.3554 mL 4.7109 mL 11.7772 mL
10 mM 0.2355 mL 1.1777 mL 2.3554 mL 5.8886 mL
15 mM 0.1570 mL 0.7851 mL 1.5703 mL 3.9257 mL
20 mM 0.1178 mL 0.5889 mL 1.1777 mL 2.9443 mL
25 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3554 mL
30 mM 0.0785 mL 0.3926 mL 0.7851 mL 1.9629 mL
40 mM 0.0589 mL 0.2944 mL 0.5889 mL 1.4721 mL
50 mM 0.0471 mL 0.2355 mL 0.4711 mL 1.1777 mL
60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9814 mL
80 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7361 mL
100 mM 0.0236 mL 0.1178 mL 0.2355 mL 0.5889 mL
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Camicinal 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:

Camicinal923565-21-3GSK962040GSK 962040GSK-962040Motilin ReceptorMLNRInhibitorinhibitorinhibit

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