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U-104

Cat. No. M3099
U-104 Structure
Synonym:

MST-104

Size Price Availability Quantity
10mg USD 60  USD60 In stock
25mg USD 120  USD120 In stock
50mg USD 185  USD185 In stock
100mg USD 340  USD340 In stock
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Quality Control & Documentation
Biological Activity

U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM, respectively, very low inhibition for CA I and CA II.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Balb/c mice orthotopically implanted with 4T1 cells.
Formulation 55.6% PEG 400, 11.1% ethanol and 33% water
Dosages 5 mg/mL
Administration Oral gavage
Chemical Information
Molecular Weight 309.32
Formula C13H12FN3O3S
CAS Number 178606-66-1
Form Solid
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tilman Todenhfer, et al. Evaluation of carbonic anhydrase IX as a potential therapeutic target in urothelial carcinoma

[2] Tanu Sharma, et al. Appraisal of groundwater quality and associated risks in Mansa district (Punjab, India)

[3] Miglė Paškevičiūtė, et al. Application of carbonic anhydrase inhibitors to increase the penetration of doxorubicin and its liposomal formulation into 2D and 3D triple negative breast cancer cell cultures

[4] Kaye J Williams, et al. Preclinical Evaluation of Ureidosulfamate Carbonic Anhydrase IX/XII Inhibitors in the Treatment of Cancers

[5] Xiaoshan Xu, et al. Association between SOX9 and CA9 in glioma, and its effects on chemosensitivity to TMZ

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Keywords: U-104, MST-104 supplier, Carbonic Anhydrase, inhibitors, activators

 
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