PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor withK_is of 0.17 nM and 1 nM for human BB₁and BB₂receptors, and 0.66 nM, 16 nM for Rat BB₁and BB₂receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), withEC₅₀s of 0.31 and 0.66 μM in HL-60 cells.

Ki: 0.17 nM (Human BB₁receptor), 0.66 nM (Rat BB₁receptor), 1 nM (Human BB₂receptor), 16 nM (Rat BB₂receptor)^[1]
EC50: 0.31 μM (FPR1), 0.66 μM (FPR2)^[2]

PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor with K_is of 0.17 nM and 1 nM for human BB₁and BB₂receptors, and 0.66 nM, 16 nM for Rat BB₁and BB₂receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB₁or BB₂receptors expressed in CHO cells, with the appK_Bs of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB₁or BB₂receptors, with appK_Bs of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC₅₀s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca²⁺mobilization in HL-60 cells transfected with human FPRs (EC₅₀, 0.72 ± 0.21 μM)^[2]. PD176252 inhibits little specific¹²⁵I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC₅₀of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC₅₀s of 7 and 5 μM^[3].

PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice^[3].

584.67

Solid

C₃₂H₃₆N₆O₅

204067-01-6

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

DMSO : 115 mg/mL(196.69 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 (stored under nitrogen)。-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: 5.75 mg/mL (9.83 mM); Suspended solution; Need ultrasonic

  此方案可获得 5.75 mg/mL (9.83 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 57.5 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%corn oil

  Solubility: ≥ 5.75 mg/mL (9.83 mM); Clear solution

  此方案可获得 ≥ 5.75 mg/mL (9.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。