AZD 4017
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $1750 | To Be Confirmed |
| 200mg | $2625 | To Be Confirmed |
| 500mg | $4430 | To Be Confirmed |
: Cat #: V4237 CAS #: 1024033-43-9 Purity ≥ 98%
Description: 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.
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| Molecular Weight (MW) | 419.58 |
|---|---|
| Molecular Formula | C22H33N3O3S |
| CAS No. | 1024033-43-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(O)C[C@H]1CN(C2=NC(SCCC)=C(C(NC3CCCCC3)=O)C=C2)CCC1 |
| Synonyms | AZD4017; AZD-4017; AZD 4017 |
| Protocol | In Vitro | AZD 4017 displays excellent selectivity versus the related enzymes 11-βHSD2, 17β-HSD1, 17β-HSD3 (all IC50>30 μM) and shows no measurable activity against the glucocorticoid and mineralocorticoid receptors. Despite having high potency for the human form of 11β-HSD1, AZD 4017 shows much reduced activity across species with the exception of cynomolgous monkey (IC50=0.029 μM). Additionally, as it is believed that adipose is a key target organ, inhibition of 11β-HSD1 activity is measured in isolated human adipocytes from nondiabetic volunteers. AZD 4017 is shown to be a potent inhibitor in this key target tissue (IC50=0.002 μM) in good agreement with the enzyme potency, thus providing some confidence that AZD 4017 is not restricted from adipose tissue by the fact that it was acidic. |
|---|---|---|
| In Vivo | Since AZD 4017 has lower potency against the mouse enzyme, only a limited number of preclinical pharmacodynamic measurements are performed. Increasing the dose further led to a maximal effect of approximately 70% inhibition at 1500 mg/kg, equivalent to 10×IC50 in the mouse, demonstrating the dose dependent inhibition of 11β-HSD1 by AZD 4017 in this model. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3833 mL | 11.9167 mL | 23.8334 mL | 47.6667 mL |
| 5mM | 0.4767 mL | 2.3833 mL | 4.7667 mL | 9.5333 mL |
| 10mM | 0.2383 mL | 1.1917 mL | 2.3833 mL | 4.7667 mL |
| 20mM | 0.1192 mL | 0.5958 mL | 1.1917 mL | 2.3833 mL |
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