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 BB₁ and BB₂ receptors, and 0.66 nM, 16 nM for Rat BB₁ and BB₂ receptors, 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.

Ki: 0.17 nM (Human BB₁ receptor), 0.66 nM (Rat BB₁ receptor), 1 nM (Human BB₂ receptor), 16 nM (Rat BB₂ receptor)^[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 BB₁ and BB₂ receptors, and 0.66 nM, 16 nM for Rat BB₁ and BB₂ receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB₁ or BB₂ receptors 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 BB₁ or BB₂ receptors, 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 specific ¹²⁵I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC₅₀ of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC₅₀s of 7 and 5 μM^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

584.67

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)

In Vitro: 

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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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
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。

• [1]. Ashwood V, et al. PD 176252–the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.

  [2]. Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90.

  [3]. Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9.

Growth studies in vitro are conducted using the MTT colorimetic assays. NCI-H1299 cells (10⁴/well) are placed in SIT medium and various concentrations of PD176252 or PD168368 added. After 4 days, MTT is added. After 4 h, 150 μL of DMSO is added. After 16 h, the optical density at 570 nm is determined^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[3]
Female athymic Balb/c nude mice, 4-5 weeks old, are housed in a pathogen-free temperature controlled isolation room, with a diet consisting of autoclaved rodent chow and autoclaved water given ad libitum. NCI-H1299 cells (1×10⁷) are injected into the right flank of each mouse by subcutaneous injection. Palpable tumors are observed in approximately 90% of the mice after 1 week. Polyethylene glycol (PEG, 100 μL) or PD176252 (10 or 1 μg in 100 μL of PEG 400) are injected daily by gavage. The tumor volume (height×width×depth) is determined weekly by calipers and recorded^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Ashwood V, et al. PD 176252–the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.

  [2]. Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90.

  [3]. Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9.