CAS NO: | 120128-20-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | RG-12525 is a a specific, competitive and orally effective antagonist of thepeptidoleukotrienes,LTC4,LTD4andLTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, withIC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also aperoxisome proliferator-activated receptorgamma (PPAR-gamma) agonist withIC50of appr 60 nM and a potent inhibitor ofCYP3A4, with a Kivalue of 0.5 μM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | RG 12525 competitively inhibits3H-LTD4 binding to lung membranes (Ki= 3.0 +/- 0.3 nM) and competitively antagonizes the spasmogenic activity of LTC4, LTD4 and LTE4 on lung strips (KB values = 3 nM) with greater than 8000 fold selectivity[1]. RG 12525 (2.5 μM or 25 μM) inhibits the microsomal activity of CYP2C9 and -3A4, but does not significantly inhibit CYP1A2,-2A6, -2C19, or -2D6. RG 12525 (25 μM) also causes a substantial amount of inhibition at the 5 and 10 μM midazolam concentrations[2]. | ||||||||||||||||
体内研究 (In Vivo) | RG 12525 orally inhibits LTD4 induced wheal formation (ED50= 5 mg/kg with a t1/2= 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED50= 0.6 mg/kg), and anaphylactic death (ED50= 2.2 mg/kg with a t1/2= 7 hrs at 10 mg/kg) and antigen induces bronchoconstriction (ED50= 0.6 mg/kg)[1]. RG 12525 inhibits antigen-induced mortality in the systemic anaphylaxis model with an ED50(95% confidence interval) = 2.2 (0.8-6.4) mg/kg. RG 12525 also protects against LTD4-induced bronchoconstriction in a model measuring changes in pulmonary function with an ED50= 0.6 (0.4-1.0) mg/kg[3]. | ||||||||||||||||
分子量 | 423.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H21N5O2 | ||||||||||||||||
CAS 号 | 120128-20-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(59.04 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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