K-604 dihydrochloride, Inhibitor | K-604, inhibitor

K-604 dihydrochloride

Cat. Num. AAA5753356

• Purity: 98.00%
• Synonyms: K-604 dihydrochloride; K-604; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 62.5mg/mL (108.57mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C23H32Cl2N6OS3
• SMILES: O=C(NC1=C(SC)C=C(C)N=C1SC)CN2CCN(CCSC3=NC4=CC=CC=C4N3)CC2.[H]Cl.[H]Cl
• CAS Number: 217094-32-1
• Target & IC50: ACAT-1: ic50 0.45uM; ACAT-2: ic50 102.85uM
• In Vitro: Administration of K-604 does not affect body weight or food consumption. The plasma cholesterol levels in fat-fed hamsters are ~12-fold higher than those in chow-fed hamsters, which are significantly decreased by K-604 only at the highest dose tested (30mg/kg) but not at lower doses (1-10mg/kg). The fatty streak lesions stain with oil red O are markedly induced by the high-fat diet, which is significantly reduced by administration of K-604. Further, the histological analyses of the atherosclerotic lesions are performed. The fatty streak lesions in the control group are characterized by accumulation of foamy macrophages in the subendothelial space. In contrast, the areas occupied by foamy macrophages are markedly reduced by administration of K-604.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for K-604, inhibitor

K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 inhibitor with an IC50 of 0.45+/-0.06uM.

References

Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7.
Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7.
Shibuya Y, et al. Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage. Neurobiol Aging. 2015 Jul;36(7):2248-2259.
Shibuya Y, et al. Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage. Neurobiol Aging. 2015 Jul;36(7):2248-2259.