| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
AG-045572 (10 μM for 40 minutes in human liver microsomes; 10 μM for 10 minutes in male rat liver microsomes; 1 μM for 10 minutes in female rat liver microsomes) in mango and The Km values in female human columnar granules, female human microsomes, and expressed CYP3A4 and CYP3A5 were similar (0.39, 0.27, 0.28, 0.25, and 0.26 μM, respectively); however, the Km value in columnar granules was 1.5 μM, indicating AG-045572 Motility and female status are supported in vivo by distinct CYP3A isoenzymes [1].
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| ln Vivo |
AG-045572, once administered at 10 mg/kg (iv) or 20 mg/kg (po), for complete loads displayed the majority of T1/2, CL, and Vss, but the Atlantic bioavailability for Female proportions have the highest bioavailability (24%), and female proportions also have similar pharmacokinetics for female injections [1]. AG-045572 (40 mg/kg twice day for three days in a female ratio) Male rats had scrotal castration surgery while under halothane anesthesia, and they were also given the opportunity to undergo this procedure. Apply halothane anesthesia during surgical castration, and permit male rats to undergo the procedure via the scrotal route. Pre- and post-study recuperation periods of 14 days [1].
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| Animal Protocol |
Animal/Disease Models: Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study[1]
Doses: 10 mg/kg, 20 mg/kg; 40 mg/kg Route of Administration: administered acutely at 10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time; For multiple-dose pretreatment, male rats at 40 mg/kg, i.m. twice a day for 3 days Experimental Results: demonstrated medium T1/2, CL and Vss but oral bioavailability was low, in female rats the bioavailability was much higher (24%) Became similar to those in female and castrated male rats. |
| References |
| Molecular Formula |
C30H37NO5
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|---|---|
| Molecular Weight |
491.63
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| Exact Mass |
491.267
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| Elemental Analysis |
C, 73.29; H, 7.59; N, 2.85; O, 16.27
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| CAS # |
263847-55-8
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| PubChem CID |
9957278
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| Appearance |
White to off-white solid powder
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| LogP |
6.878
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
740
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C(C)(C)CCC2(C)C)C=C1CC1OC(C(NC2C(OC)=CC(OC)=CC=2OC)=O)=CC=1
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| InChi Key |
IPEMCIBPDYCJLO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H37NO5/c1-18-13-22-23(30(4,5)12-11-29(22,2)3)15-19(18)14-20-9-10-24(36-20)28(32)31-27-25(34-7)16-21(33-6)17-26(27)35-8/h9-10,13,15-17H,11-12,14H2,1-8H3,(H,31,32)
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| Chemical Name |
5-[5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl-methyl]-N-(2,4,6-trimethoxyphenyl)-2-furancarboxamide
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| Synonyms |
AG-045572, AG045572, AG 045572
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0340 mL | 10.1702 mL | 20.3405 mL | |
| 5 mM | 0.4068 mL | 2.0340 mL | 4.0681 mL | |
| 10 mM | 0.2034 mL | 1.0170 mL | 2.0340 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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