| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following a single oral administration, this product is rapidly and extensively absorbed in the human body, with an absolute bioavailability of 48%. Incomplete bioavailability is due to incomplete absorption and the first-pass effect in the liver. Metabolism/Metabolites Cytochrome P450 (CYP) 3A4/5 and CYP2C9 participate in the metabolism of dexloxigramiylate to O-desmethyldexloxigramiylate. This metabolite is further oxidized to dexloxigramiic acid. These two major metabolites have been identified (accounting for 50% of dexloxigramiylate elimination). However, in human plasma, the parent drug is the major component of the metabolic profile (up to 91%). The parent drug is considered the main contributor to the efficacy of this compound because its major metabolites are not pharmacologically active. The known human metabolites of deloxigramid include 4-[(3,4-dichlorobenzoyl)amino]-5-[3-hydroxypropyl(pentyl)amino]-5-oxovalerate. |
|---|---|
| Toxicity/Toxicokinetics |
Protein Binding
94-98% |
| References |
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| Additional Infomation |
Dexloxiglumide is a glutamate derivative. Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist, currently undergoing Phase III clinical trials only in Europe by Rottapharm, as its trials in the United States have been terminated. As the D-isomer of loxigrammet, it retains all the pharmacological properties of loxigrammet but is more potent. Indications: For the treatment of irritable bowel syndrome (IBS) and gastroesophageal reflux disease (GERD). Mechanism of Action: CCKA antagonists target receptors in the gastrointestinal system to promote gastric emptying and intestinal motility, and modulate intestinal sensitivity to distension.
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| Molecular Formula |
C21H30N2O5CL2
|
|---|---|
| Molecular Weight |
461.3793
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| Exact Mass |
460.153
|
| CAS # |
119817-90-2
|
| PubChem CID |
65937
|
| Appearance |
White to off-white solid powder
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| Density |
1.233g/cm3
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| Boiling Point |
632.2ºC at 760mmHg
|
| Flash Point |
336.1ºC
|
| Vapour Pressure |
7.51E-17mmHg at 25°C
|
| Index of Refraction |
1.537
|
| LogP |
4.402
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
30
|
| Complexity |
550
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CCCCCN(CCCOC)C(=O)[C@@H](CCC(=O)O)NC(=O)C1=CC(=C(C=C1)Cl)Cl
|
| InChi Key |
QNQZBKQEIFTHFZ-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C21H30Cl2N2O5/c1-3-4-5-11-25(12-6-13-30-2)21(29)18(9-10-19(26)27)24-20(28)15-7-8-16(22)17(23)14-15/h7-8,14,18H,3-6,9-13H2,1-2H3,(H,24,28)(H,26,27)/t18-/m1/s1
|
| Chemical Name |
(4R)-4-[(3,4-dichlorobenzoyl)amino]-5-[3-methoxypropyl(pentyl)amino]-5-oxopentanoic acid
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| 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 |
| 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) |
DMSO : ~50 mg/mL (~108.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.42 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1674 mL | 10.8371 mL | 21.6741 mL | |
| 5 mM | 0.4335 mL | 2.1674 mL | 4.3348 mL | |
| 10 mM | 0.2167 mL | 1.0837 mL | 2.1674 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.
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