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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
A922500 (A-922500; A 922500) is a selective and orally bioactive inhibitor for human/mouse acyl CoA/diacylglycerol acyltransferase(DGAT-1) with anti-hyperlipidemic effects. It inhibits DGAT-1 with IC50s of 7 nM and 24 nM, respectively. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in diet-induced obesity-DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice.
| ln Vitro |
A922500 (A-922500) exhibits remarkable selectivity compared to other acyltransferases, such as DGAT-2 (IC50=53 μM) and the members of the phylogenetic family, acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50=296 μM) [1].
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| ln Vivo |
At all studied dosages, the DGAT-1 inhibitor A 922500 (A-922500) lowers blood triglyceride levels from baseline; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53% on average. Similarly, serum FFA concentrations are considerably reduced by 55% and total cholesterol by 25% with the 3 mg/kg dose of A 922500. No studied dose of DGAT-1 inhibition significantly affects body weight. A 922500 at 0.3 and 3 mg/kg considerably improves the blood LDL/HDL-cholesterol ratio, even though it has little effect on LDL or HDL cholesterol individually. Treated with 3 mg/kg A 922500, blood triglyceride concentrations are dramatically reduced (39%), just as in the dyslipidemic hamster. In animals treated with vehicles, FFA levels rise dramatically over the course of 14 days. A 922500 inhibits this rise in a dose-dependent manner, resulting in 32% lower FFA concentrations after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg when compared to the vehicle group (p < 0.05). A 922500 raises HDL-cholesterol from baseline levels considerably at doses of 0.3 and 3 mg/kg; however, this rise is only significant when compared to the vehicle at the 3 mg/kg dose. In rats treated with vehicles, body weight increases dramatically over a 2-week period; A 922500 has no effect on this. In the group receiving vehicle treatment, LDL cholesterol is much lower. Both LDL and total cholesterol are not further decreased by DGAT-1 inhibition[1].
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| Animal Protocol |
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| Additional Infomation |
A 922500 is an aromatic ketone.
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| Molecular Formula |
C26H24N2O4
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| Molecular Weight |
428.48
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| Exact Mass |
428.173
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| CAS # |
959122-11-3
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| Related CAS # |
959122-11-3;
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| PubChem CID |
24768261
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
576.1±50.0 °C at 760 mmHg
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| Flash Point |
302.2±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
4.77
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
659
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C[C@H]([C@@H](C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4
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| InChi Key |
BOZRFEQDOFSZBV-DHIUTWEWSA-N
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| InChi Code |
InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
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| Chemical Name |
(1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 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: 15% Captisol: 20mg/mL View More
Solubility in Formulation 3: 6.67 mg/mL (15.57 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3338 mL | 11.6692 mL | 23.3383 mL | |
| 5 mM | 0.4668 mL | 2.3338 mL | 4.6677 mL | |
| 10 mM | 0.2334 mL | 1.1669 mL | 2.3338 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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