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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $198 | 1-2 weeks | 1-2 weeks | |
| 5 mg | $347 | 1-2 weeks | 1-2 weeks | |
| 25 mg | $1,140 | 1-2 weeks | 1-2 weeks | |
| 50 mg | $1,490 | 1-2 weeks | 1-2 weeks | |
| 100 mg | $1,990 | 1-2 weeks | 1-2 weeks | |
| 1 mL x 10 mM (in DMSO) | $382 | 1-2 weeks | 1-2 weeks |
| 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. |
| Synonyms | GSK962040 |
| Molecular Weight | 424.55 |
| Formula | C25H33FN4O |
| Cas No. | 923565-21-3 |
| Smiles | C[C@H]1CN(Cc2ccc(CC(=O)N3CCC(CC3)Nc3cccc(F)c3)cc2)CCN1 |
| Relative Density. | 1.175 g/cm3 (Predicted) |
| Storage | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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