| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| ln Vitro |
AZD3988 (compound 53) has an IC50 value of 0 and can inhibit DGAT-1 at 10 μM. Human: 6 nM, 0. 0.5 nM (HuTu 80 cells), 1.1 nM (mouse), and 5 nM (rat) [1].
|
|---|---|
| ln Vivo |
AZD3988 (compound 53) exhibits good in vivo pharmacokinetic effectiveness (iv, po; 0.5, 1, 2, 5 mg/kg) [1].
|
| Animal Protocol |
Animal/Disease Models: Mice, rats and dogs [1]
Doses: 0.5, 1, 2, 5 mg/kg Route of Administration: intravenous (iv) (iv)injection of 0.5 mg/kg (mouse), 2 mg/kg (rat) and 1 mg/kg (dog) and orally 1 mg/kg (mouse), 5 mg/kg (rat) and 1 mg/kg (dog) Experimental Results: Species Clp (mL/min/kg) Vdss(L/kg) IV Half-life (h) po Half-life (h) po Cmax (lM) Bioavailability (%) Mice 4.6 0.99 4.9 4.7 1.9 >100 Rats 1.1 0.35 3.4 5.8 20 >100 Dogs 2.5 0.36 1.8 5.7 1.5 32 Oral Lipid Tolerance Test (OLTT) in Rats:** Fasted rats were orally dosed with AZD3988 (0.03, 0.1, 0.2 mg/kg) or vehicle. Two hours later, they received a bolus dose of corn oil. Plasma TAG levels were measured 1.5 hours after the oil challenge to assess the compound's effect on postprandial TAG excursion. [1] - **Adipose TAG Synthesis Assay in Rats:** Rats were dosed with AZD3988 (0.1, 0.3, 1, 3 mg/kg) or vehicle. At a specific time point (presumably after compound administration and a radiolabeled precursor), adipose tissue was collected. The ratio of radiolabel incorporated into TAG versus diacylglycerol (DAG) was measured as a marker of DGAT-1 activity in the tissue. [1] - **Diet-Induced Obesity (DIO) Mouse Study:** DIO mice on a high-energy cafeteria diet were treated with AZD3988 or vehicle twice daily (at 6:00 and 16:00) for 3 days. Body weight was measured daily. Free plasma concentrations of the compound were monitored to ensure target coverage. [1] - **Pharmacokinetic (PK) Studies:** AZD3988 was dosed intravenously (IV) and orally (PO) in mice, rats, and dogs to determine key PK parameters. Formulations included 5% DMSO:95% hydroxypropyl β-cyclodextrin for IV dosing and hydroxypropyl methylcellulose (HPMC) with 0.1% polysorbate for PO dosing. Blood samples were collected at various time points, and plasma concentrations were analyzed. [1] |
| References |
| Molecular Formula |
C23H22F2N4O4
|
|---|---|
| Molecular Weight |
456.44
|
| Exact Mass |
456.161
|
| CAS # |
892489-52-0
|
| PubChem CID |
23648867
|
| Appearance |
White to off-white solid powder
|
| Density |
1.402
|
| Index of Refraction |
1.627
|
| LogP |
5.238
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
33
|
| Complexity |
671
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NGEBYTLALFOQKI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H22F2N4O4/c24-18-10-9-17(12-19(18)25)27-23-29-28-22(33-23)21(32)26-16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-20(30)31/h5-10,12-14H,1-4,11H2,(H,26,32)(H,27,29)(H,30,31)
|
| Chemical Name |
2-[4-[4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl]cyclohexyl]acetic acid
|
| Synonyms |
AZD3988 AZD 3988 AZD-3988
|
| 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 : ~16.67 mg/mL (~36.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 16.7 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. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.66 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 16.7 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 | 2.1909 mL | 10.9543 mL | 21.9087 mL | |
| 5 mM | 0.4382 mL | 2.1909 mL | 4.3817 mL | |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1909 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
