Azamulin (Synonyms: Antibiotic TDM 85-530) |
Catalog No.GC42888
One-Click Copy Product Info
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Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 76530-44-4
Sample solution is provided at 25 µL, 10mM.
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Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources). [1] It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. [1] Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.[2]
Reference:
[1]. Stresser, D.M., Broudy, M.I., Ho, T., et al. Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metabolism and Disposition 32(1), 105-112 (2004).
[2]. Lim, H.K., Duczak, N., Jr., Brougham, K., et al. Automated screening with confirmation of mechanism-based inactivation of CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP1A2 in pooled human liver microsomes. Drug Metabolism and Disposition 33(8), 1211-1219 (2005).
| Cas No. | 76530-44-4 | SDF | |
| Synonyms | Antibiotic TDM 85-530 | ||
| Chemical Name | (3aS,4R,5S,6R,8R,9R,9aR,10R)-6-ethyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester 2-[(3-amino-1H-1,2,4-triazol-5-yl)thio]-acetic acid | ||
| Canonical SMILES | O=C1CC[C@@]23[C@@H](C)[C@H](O)[C@@](CC)(C)C[C@@H](OC(CSC4=NN=C(N)N4)=O)[C@](C)([C@H](C)CC3)[C@@]21[H] | ||
| Formula | C24H38N4O4S | M.Wt | 478.7 |
| Solubility | 20mg/mL in ethanol, or in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.089 mL | 10.445 mL | 20.8899 mL |
| 5 mM | 417.8 μL | 2.089 mL | 4.178 mL |
| 10 mM | 208.9 μL | 1.0445 mL | 2.089 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)