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商品描述
CWHM-12
- Catalog No.:MC1099
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo:
- 1564286-55-0
- MolecularFormula:
- C26H32BrN5O6
- Purity:
- >98%
- Target:
- Integrin
- IC50:
- IC50: 0.2 nM (αvβ8), 0.8 nM (αvβ3), 1.5 nM (αvβ6), 1.8 nM (αvβ1), 61 nM (αvβ5)[1]
- In Vitro:
- CWHM-12 (CWHM 12) also less potently inhibits αvβ5 (IC50=61 nM) and αIIbβ3/α2β1/α10β1 (IC50>5000 nM). 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, with somewhat less potency against αvβ5 than against the other αv integrins[1].
- In Vivo:
- Mice are treated with CCl4 for 3 weeks to establish fibrotic disease and then treated with CWHM-12 (CWHM 12) or vehicle for the final 3 weeks of CCl4. 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[1].
- Fields:
- CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.
- Specificity:
- Target:Integrin. Fields: CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2
- Source:
- Rabbit
- Dilution:
- IC50: 0.2 nM (αvβ8), 0.8 nM (αvβ3), 1.5 nM (αvβ6), 1.8 nM (αvβ1), 61 nM (αvβ5)[1]
- Concentration:
- >98%
- Storage Stability:
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name:
- CWHM 12,CWHM12
- MolecularWeight(Da):
- 590.47
- References:
- [1]. Henderson NC, et al. Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs. Nat Med. 2013 Dec;19(12):1617-24.
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