BMS 193885 是一种选择性和竞争性神经肽 Y(1) 受体拮抗剂,亲和力为 3.3 nM。
产品描述
BMS 193885 is a selective and competitive neuropeptide Y(1) receptor antagonist with affinity of 3.3 nM.
体外活性
BMS 193885 increases the Kd of [(125)I]PeptideYY from 0.35 nM to 0.65 nM without changing the Bmax (0.16 pmol/mg of protein) in SK-N-MC cells that endogenously express the neuropeptide Y(1) receptor[1]. BMS 193885 is a full antagonist with an apparent Kb of 4.5 nM measured by reversal of forskolin-stimulated inhibition of cAMP production by neuropeptide Y[1].
体内活性
BMS 193885 (10 mg/kg; i.p.) reduces one-hour neuropeptide Y-induced food intake in satiated rats, as well as spontaneous overnight food consumption. Chronic administration of BMS 193885 (10 mg/kg) i.p. for 44 days significantly reduces food intake and the rate of body weight gain compared to vehicle treated control without developing tolerance or affecting water intake[1].
Cas No.
679839-66-8
分子式
C36H48N4O9
分子量
680.79
别名
BMS193885
储存和溶解度
H2O:<13.62mg/ml
DMSO:<68.08mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years