Astressin acetate 是促肾上腺皮质激素释放因子 (CRF) 的拮抗剂,对 CRF 结合蛋白具有低亲和力,对克隆垂体受体具有高亲和力 (Ki = 2 nM)。
产品描述
Astressin acetate is an antagonist of corticotropin releasing factor (CRF) with low affinity for the CRF binding protein and high affinity for the cloned pituitary receptor(Ki = 2 nM).
体外活性
Astressin acetate exhibits high affinity for cloned human CRF-RA1 stably expressed in CHO cells and high potency to inhibit ACTH secretion[2].
体内活性
Astressin acetate (i.c.v. 30 min before and 10 min after seizures) decreases damage in some hippocampal cell fields by as much as 84%. Astressin acetate protects even if administered only 10 min following excitotoxin exposure[1]. Astressin acetate is significantly more potent than any previously tested antagonist in reducing hypophyseal corticotropin secretion in stressed or adrenalectomized rats. Astressin acetate (30 and 100 μg/kg; i.v.) produces a significant decrease in ACTH levels at 45 and 90 min, respectively[2]. Astressin acetate significantly reverses the anxiogenic-like response induced by both social stress and i.c.v. rat/humanCRF (r/hCRF) on the elevated plus-maze, but fails to block the effects of r/hCRF-induced locomotor activity in a familiar environment[3].
Cas No.
TP1448L
分子式
C163H273N49O44
分子量
3623.21
别名
Astressin acetate (170809-51-5 Free base)
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years