?-GLUCURONIDASE INHIBITOR 1PC X 10MG (C005B-227440)

General description

An orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC₅₀ = 283 nM; k_cat/K_m = 0.0987 s^-1µM^-1; K_i = 164 nM in vitro assays against E coli β-glucuronidase; EC₅₀ = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>>100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wallace, B.D., et al. 2010. Science330, 831.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 425.54. Empirical Formula: C₂₃H₂₇N₃O₃S. Quality Level: 100. Assay: ≥. 99% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: O: C(N1)C(CN(C(NC2: CC: C(C: C2)OCC): S)CCO): CC3: C1C(C): CC(C): C3. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.

Shipping Information:

Dry Ice Surcharge & Ice Pack Shipments: $40

More Information: https://cenmed.com/shipping-returns

UPC:

12352200

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

10

Unit of Measurement:

MG

MPN:

347423-10MG

Temperature Control Device:

Yes