CAS NO: | 186371-96-0 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
生物活性 | ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3analog and a pureVDRantagonist with aKdvalue of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor[1]. | ||||||||||||||||
IC50& Target | Kd: 0.1 nM (VDR)[1] | ||||||||||||||||
体外研究 (In Vitro) | ZK168281 resembles more the mouse constitutive androstane receptor (CAR) inverse agonist Androstanol in its ability to recruit corepressor (CoR) proteins. A salt bridge between the CoR and a conserved lysine in helix 4 of the nuclear receptor (NR) is central to this interaction, but also helix 12 was stabilized by direct contacts with residues of the CoR. Fixation of helix 12 in the antagonistic/inverse agonistic conformation prevents an energetically unfavorable free floatation of the C terminus[1]. | ||||||||||||||||
分子量 | 510.70 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C32H46O5 | ||||||||||||||||
CAS 号 | 186371-96-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(195.81 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |