CWHM-12

Research use only, not for human use.

A novel active RGD peptidomimetic inhibitor of αv integrin with IC50s of 1.8/0.8/61/1.5/0.2 nM for αvβ1/αvβ3/αvβ5/αvβ6/αvβ8; no inhibition on αIIbβ3, α2β1 and α10β1 (>50 uM).

A novel active RGD peptidomimetic inhibitor of αv integrin with IC50s of 1.8/0.8/61/1.5/0.2 nM for αvβ1/αvβ3/αvβ5/αvβ6/αvβ8; no inhibition on αIIbβ3, α2β1 and α10β1 (>50 uM); significantly inhibits progression of pulmonary fibrosis in mice model.Cystic Fibrosis Preclinical.

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.

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.

CWHM12 | CWHM 12 | CWHM-12.

Cell Cycle/DNA Damage

Integrin

Integrin

Other Indications

Fibrosis

1564286-55-0

590.4662

C26H32BrN5O6

>98% (HPLC)

DMSO: 10.5 mg/mL

OC1=CC(C(NCC(N[C@@H](CC(O)=O)C2=CC(Br)=CC(C(C)(C)C)=C2)=O)=O)=CC(NC3=NCC(O)CN3)=C1

β-Alanine, N-[3-hydroxy-5-[(1,4,5,6-tetrahydro-5-hydroxy-2-pyrimidinyl)amino]benzoyl]glycyl-3-[3-bromo-5-(1,1-dimethylethyl)phenyl]-, (3S)-

(-20℃)

With Ice Pack

≥ 2 years