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| 5mg |
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| 25mg |
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Purity: ≥98%
AZD4017, a nicotinic amide derived carboxylic acid, is a novel, potent, selective and effective inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) in human adipocytes with an IC50 of 7 nM. It exhibits good druglike properties and as a consequence was selected for clinical development. Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. AZD4017 has good potency, selectivity, and pharmacokinetic characteristics.
| ln Vitro |
AZD 4017 displays no detectable activity against glucocorticoid and mineralocorticoid receptors, but demonstrates remarkable selectivity against related enzymes 11-βHSD2, 17β-HSD1, and 17β-HSD3 (all IC50>30 μM). With the exception of cynomolgus monkeys (IC50=0.029 μM), AZD 4017 has markedly reduced activity in various species, despite its high potency against the human version of 11β-HSD1. Furthermore, as adipose tissue is believed to be an important target organ, suppression of 11β-HSD1 activity was assessed in isolated human adipocytes from individuals without diabetes. There is considerable certainty that AZD 4017 is not restricted by adipose tissue because of its acidic nature because it was demonstrated to be a strong inhibitor of this important target tissue (IC50=0.002 μM), which is in good accord with the potency of the enzyme [1].
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| ln Vivo |
Only a few preclinical pharmacodynamic evaluations were carried out because of AZD 4017's low efficacy against the mouse enzyme. Increasing the doses further produced a maximal effect of about 70% inhibition at 1500 mg/kg, which is comparable to 10×IC50 in mice. This indicates that AZD 4017 inhibits 11β-HSD1 in this model in a dose-dependent manner [1].
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| References |
[1]. Scott JS, et al. Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017). J Med Chem. 2012 Jun 28;55(12):5951-64.
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| Molecular Formula |
C22H33N3O3S
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|---|---|
| Molecular Weight |
419.58100
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| CAS # |
1024033-43-9
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| SMILES |
O=C(O)C[C@H]1CN(C2=NC(SCCC)=C(C(NC3CCCCC3)=O)C=C2)CCC1
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| 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~297.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 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 20.8 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: ≥ 2.08 mg/mL (4.96 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 20.8 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 | 2.3833 mL | 11.9167 mL | 23.8334 mL | |
| 5 mM | 0.4767 mL | 2.3833 mL | 4.7667 mL | |
| 10 mM | 0.2383 mL | 1.1917 mL | 2.3833 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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