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Camicinal

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Catalog No. T11508Cas No. 923565-21-3
Alias GSK962040

Camicinal is a selective motilin receptor agonist (pEC50: 7.9).

Camicinal

Camicinal

😃Good
Catalog No. T11508Alias GSK962040Cas No. 923565-21-3
Camicinal is a selective motilin receptor agonist (pEC50: 7.9).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$1981-2 weeks1-2 weeks
5 mg$3471-2 weeks1-2 weeks
25 mg$1,1401-2 weeks1-2 weeks
50 mg$1,4901-2 weeks1-2 weeks
100 mg$1,9901-2 weeks1-2 weeks
1 mL x 10 mM (in DMSO)$3821-2 weeks1-2 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Camicinal is a selective motilin receptor agonist (pEC50: 7.9).
Targets&IC50
Motilin receptor:(pEC50)7.9
In vitro
Camicinal ?had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal ?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 ?were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) . Camicinal ?activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal ?was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .
In vivo
Camicinal (5 mg free base kg 1) increased total fecal weight over the 2-hour post-dose period (21.2 ± 4.5 g; P < 0.05). It induced dose-related phasic contractions (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. MMC restoration was unaffected by 3 mg kg 1 GSK962040 but returned 253 min after dosing at 6 mg kg 1, compared to 101 min after saline (n = 5 each). The oral bioavailability (Fpo) of Camicinal (GSK962040) was 48 ± 13%. Camicinal had a long-lasting effect (T1/2 = 46.9 ± 5.0 min at 3 μM) compared with the short-lived effect of [Nle13]motilin (T1/2 = 11.4 ± 1.5 min at 0.3 μM). Camicinal strongly facilitated cholinergic activity in the antrum, with lower activity in the fundus and small intestine.
SynonymsGSK962040
Chemical Properties
Molecular Weight424.55
FormulaC25H33FN4O
Cas No.923565-21-3
SmilesC[C@H]1CN(Cc2ccc(CC(=O)N3CCC(CC3)Nc3cccc(F)c3)cc2)CCN1
Relative Density.1.175 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (235.54 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3554 mL11.7772 mL23.5544 mL117.7718 mL
5 mM0.4711 mL2.3554 mL4.7109 mL23.5544 mL
10 mM0.2355 mL1.1777 mL2.3554 mL11.7772 mL
20 mM0.1178 mL0.5889 mL1.1777 mL5.8886 mL
50 mM0.0471 mL0.2355 mL0.4711 mL2.3554 mL
100 mM0.0236 mL0.1178 mL0.2355 mL1.1777 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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2 Enter the in vivo formulation:
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%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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