Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
ln Vitro |
GSK962040 hydrochloride, also known as camecicinal hydrochloride, exhibits negligible effects on ghrelin and other receptors, ion channels, and enzymes. When Camicinal hydrochloride (GSK962040 hydrochloride) was administered at 300 nmol L 1-10 μmol L 1, the cholinergic-mediated contraction amplitude in the rabbit stomach antrum was prolonged and reached a maximum of 248 ± 47% at 3 μmol L 1. The following were found in the samples: 10.4±0.01 (n=770), 7.3±0.29 (n=4), and 7.9±0.09 (n=17) for motilin, erythromycin, and Camicinal hydrochloride (GSK962040 hydrochloride) [1]. Dog motilin receptor activation is caused by camicinal hydrochloride (GSK962040 hydrochloride) (pEC50 5.79; intrinsic activity 0.72 relative to [Nle13]-motilin) [2]. Because its initial IC50 value on CYP3A4 was much greater than our recommended threshold of 10 μM [3], camicinal hydrochloride (GSK962040 hydrochloride) was preferred.
|
---|---|
ln Vivo |
Camicinal (GSK962040) (5 mg free base·kg 1) also raises the overall weight of the feces after two hours after administration (21.2 ± 4.5 g; P < 0.05). [1]. Camicinal (GSK962040) causes mean plasma concentrations >1.14 μmol L 1 to cause dose-related phasic contractions that last 48 and 173 minutes for 3 and 6 mg kg 1, respectively. Migratory motor complex (MMC) activity returns when the effects of Camicinal (GSK962040) wear off. The 3 mg kg 1 Camicinal (GSK962040) had no effect on the migration of motor complex recovery; however, at the 6 mg kg 1 dose, MMC recovered 253 minutes after delivery as opposed to 101 minutes after saline (n = 5 each).[2]. The oral bioavailability (Fpo) of camicinal (GSK962040) is 48 (13%). In contrast to short-term effects, camicinal (GSK962040) demonstrated long-term effects (T1/2) 46.9 (5.0 min at 3 μM) [Nle13].Motilin (T1/2) 11.4 (at 0.3 μM) for 1.5 minutes [3]. The compound camicinal (GSK962040) is less active in the fundus and small intestine but significantly increases cholinergic activity in the gastric antrum [4].
|
References |
[1]. Sanger, G.J., et al., GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterol Motil, 2009. 21(6): p. 657-64, e30-1.
[2]. Leming, S., et al., GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs. Neurogastroenterol Motil, 2011. 23(10): p. 958-e410. [3]. Westaway, S.M., et al., Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-pi peridinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. J Med Chem, 2009. 52(4): p. 1180-9. [4]. Broad, J., et al., Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists. Br J Pharmacol, 2012. 167(4): p. 763-74. |
Molecular Formula |
C25H33N4OF.HCL
|
---|---|
Molecular Weight |
461.01506
|
CAS # |
923565-22-4
|
Related CAS # |
Camicinal;923565-21-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=C(N1CCC(NC2=CC=CC(F)=C2)CC1)CC3=CC=C(CN4C[C@H](C)NCC4)C=C3.Cl
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
H2O : ~100 mg/mL (~216.91 mM)
DMSO : ~100 mg/mL (~216.91 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (216.91 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1691 mL | 10.8455 mL | 21.6910 mL | |
5 mM | 0.4338 mL | 2.1691 mL | 4.3382 mL | |
10 mM | 0.2169 mL | 1.0846 mL | 2.1691 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.