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 K_ivalue of 0.5 μM.

RG 12525 competitively inhibits³H-LTD4 binding to lung membranes (K_i= 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].

RG 12525 orally inhibits LTD4 induced wheal formation (ED₅₀= 5 mg/kg with a t_1/2= 10 hrs at 9 mg/kg), LTD4 induces bronchoconstriction (ED₅₀= 0.6 mg/kg), and anaphylactic death (ED₅₀= 2.2 mg/kg with a t_1/2= 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].

423.47

Solid

C₂₅H₂₁N₅O₂

120128-20-3

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(59.04 mM;Need ultrasonic)

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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.91 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.08 mg/mL (4.91 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (4.91 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明