ML753286 |
Katalog-Nr.GC38129
One-Click Copy Product Info
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ML753286 ist ein oral aktiver und selektiver BCRP (Breast Cancer Resistance Protein)-Inhibitor mit einem IC50 von 0,6 μM. ML753286 hat eine hohe PermeabilitÄt und eine geringe bis mittlere Clearance in Leber-S9-Fraktionen von Nagetieren und Menschen und ist in Plasmaarten verschiedener Spezies stabil.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1699720-89-2
Sample solution is provided at 25 µL, 10mM.
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ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species[1].
ML753286 has IC50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively[1].
ML753286 (25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV); 0.083-24 hours) appears to completely inhibit Bcrp functions in rats at 25 mg/kg PO or at 20 mg/kg IV. The tmax values in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively[1]. Animal Model: Male Bcrp KO (Abcg2-/-) and WT (Wistar) Rats[1]
[1]. Liao M, et al. Preclinical absorption, distribution, metabolism, excretion and pharmacokinetics of a novelselective inhibitor of breast cancer resistance protein (BCRP). Xenobiotica. 2018 May;48(5):467-477.
| Cas No. | 1699720-89-2 | SDF | |
| Canonical SMILES | COC1=CC=C2C(NC3=C2C[C@]4(N([C@H]3CC(C)C)C([C@@H](NC4=O)C)=O)[H])=C1 | ||
| Formula | C20H25N3O3 | M.Wt | 355.43 |
| Löslichkeit | Soluble in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8135 mL | 14.0675 mL | 28.1349 mL |
| 5 mM | 562.7 μL | 2.8135 mL | 5.627 mL |
| 10 mM | 281.3 μL | 1.4067 mL | 2.8135 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)