| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
Using a recombinant human form complexed with protein disulfide isomerase, implitapide reduces MTP activity (IC50=10 nM) and inhibits the production of apoB-containing very low-density lipoprotein (VLDL)-like lipids by human hepatoma cells (HepG2) with an IC50 value. Protein at 1.1 nM [1].
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| ln Vivo |
Implitapide (3.2 mg/kg/d) significantly lowered plasma lipid levels to levels near to or below dietary (CD) levels after 4 and 8 weeks of therapy (p<0.01). Implitapide (3.2 mg/kg/d) effectively reduces lipid-stained lesions in Western diet (WD)-fed mice. Compared with the WD group, Inprotapid (3.2 mg/kg/d) significantly reduced the lesion area by 83% (p<0.01). Feeding WD ApoE KO mice for 14 weeks containing imprecitap (1, 5, and 15 mg/kg/d) has been demonstrated to dramatically reduce plaque area (66%, 78%, and 93%, respectively). and lipid percentage within the plaque (4.3, 2.6, and 0%, respectively, compared with 9.5% in the control group). In apoE KO mice, Implitapide at a dose of roughly 3.2 mg/kg/d dramatically decreased lipid-stained aortic lesions by 83% [1].
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| References | |
| Additional Infomation |
Implitapide is a microsomal triglyceride transfer protein (MTP)-inhibitor.
Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions. Drug Indication For the treatment of atherosclerosis. Mechanism of Action MTP mediates triglyceride absorption and chylomicron secretion from the intestine and very-low-density lipoprotein (VLDL) secretion from the liver by linking lipid molecules with apolipoprotein B (apoB). Inhibition of MTP reduces the level of all apoB-containing lipoproteins, including LDL. |
| Molecular Formula |
C35H37N3O2
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|---|---|
| Molecular Weight |
531.7
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| Exact Mass |
531.288
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| CAS # |
177469-96-4
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| Related CAS # |
Implitapide Racemate;177277-99-5
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| PubChem CID |
5745206
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
739.3±60.0 °C at 760 mmHg
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| Flash Point |
400.9±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.653
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| LogP |
6.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
40
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| Complexity |
824
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC(=NC2=C1C3=CC=CC=C3N2CC4=CC(=CC=C4)[C@H](C5CCCC5)C(=O)N[C@@H](CO)C6=CC=CC=C6)C
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| InChi Key |
AMNXBQPRODZJQR-DITALETJSA-N
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| InChi Code |
InChI=1S/C35H37N3O2/c1-23-19-24(2)36-34-32(23)29-17-8-9-18-31(29)38(34)21-25-11-10-16-28(20-25)33(27-14-6-7-15-27)35(40)37-30(22-39)26-12-4-3-5-13-26/h3-5,8-13,16-20,27,30,33,39H,6-7,14-15,21-22H2,1-2H3,(H,37,40)/t30-,33-/m0/s1
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| Chemical Name |
(2S)-2-cyclopentyl-2-[3-[(2,4-dimethylpyrido[2,3-b]indol-9-yl)methyl]phenyl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
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| Synonyms |
BAY-139952 BAY-13-9952 AEGR-427
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~188.08 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8808 mL | 9.4038 mL | 18.8076 mL | |
| 5 mM | 0.3762 mL | 1.8808 mL | 3.7615 mL | |
| 10 mM | 0.1881 mL | 0.9404 mL | 1.8808 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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