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CWHM-12

Cat. No. M8975
CWHM-12 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 250 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CWHM-12 is a potent inhibitor of αV integrins with IC50 values of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1, respectively. CWHM-12 demonstrates high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assays.

In vivo, CWHM-12 significantly reduces liver fibrosis even after fibrotic disease have been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compare to controls, demonstrating that the protection from CCl4-induced hepatic fibrosis observed in CWHM-12 treated mice is due at least in part to a reduction in TGF-β activation by αv integrins. Besides, administration of CWHM-12 significantly inhibited progression of pulmonary fibrosis.

Protocol
Cell Experiment
Cell lines The stably transfected human 293 cells over-expressing human αvβ3 or αvβ5
Preparation method The stably transfected human 293 cells over-expressing human αvβ3 or αvβ5 are pre-incubated in HBSS buffer containing 200 μM MnCl2 for 30 min at 37°C with 3-fold dilutions of compound (e.g., CWHM-12). Each sample is then added to triplicate wells of a 96-well plate which has been coated overnight at 4°C with a predetermined optimal concentration of purified vitronectin, washed, blocked by 1 hr incubation with BSA, and washed again. Cells are allowed to attach for 30 min at 37°C, and non-adherent cells are removed by washing. Remaining attached cells are measured by endogenous alkaline phosphatase activity using para-nitrophenyl phosphate and reading absorbance signal at 405 nM.
Concentrations
Incubation time 90 min
Animal Experiment
Animal models Wild type C57/BL6 mice, Itgav(flox/flox) mice and itgb8(flox/flox) mice
Formulation 50% DMSO (in sterile water)
Dosages 100 mg/kg/day
Administration delivered by implantable ALZET osmotic minipumps
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 590.47
Formula C26H32BrN5O6
CAS Number 1564286-55-0
Purity >98%
Solubility DMSO: 10 mg/mL
Storage at -20°C
References

Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs.
Henderson NC, et al. Nat Med. 2013 Dec;19(12):1617-24. PMID: 24216753.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CWHM-12 supplier, Integrin, inhibitors

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