1. GPCR/G Protein
  2. Bombesin Receptor
  3. PD 168368

PD 168368 是一种有效的、竞争性的选择性神经调节蛋白 B 受体 (NMB-R) 拮抗剂,Ki 为 15-45 nM。 PD 168368 是神经调节素 B 受体(NMBR; IC50=96 nM)和胃泌素释放肽受体 (GRPR; IC50=3500 nM))的双重拮抗剂。PD 168368 还是一种 FPR1/FPR2/FPR3 的混合激动剂,EC50 分别为 0.57、0.24 和 2.7 nM。

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PD 168368 Chemical Structure

PD 168368 Chemical Structure

CAS No. : 204066-82-0

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].

体外研究
(In Vitro)

PD 168368 (PD168368) is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range[3].
PD 168368 (PD168368) suppresses migration and invasion of the human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation. PD 168368 (5 μM) inhibits migration and invasiveness in breast cancer cells[4].
PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: Human breast cancer cell line MDA-MB-231
Concentration: 5 μM
Incubation Time: 24 hours
Result: Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay.

Cell Viability Assay[4]

Cell Line: MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 0, 0.5, 1, 2, 4, 8, and 16 hours
Result: Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner.
体内研究
(In Vivo)

PD 168368 (PD168368) potently inhibits in vivo metastasis of breast cancer. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits metastasis of breast cancer in mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model[4]
Dosage: 1.2 mg/kg
Administration: Intraperitoneal injection for 30 days
Result: No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice.
分子量

554.64

Formula

C31H34N6O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 30 mg/mL (54.09 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

DMF 中的溶解度 : 10 mg/mL (18.03 mM; 超声加热助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8030 mL 9.0149 mL 18.0297 mL
5 mM 0.3606 mL 1.8030 mL 3.6059 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

PD 168368 相关分类

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMF / DMSO 1 mM 1.8030 mL 9.0149 mL 18.0297 mL 45.0743 mL
5 mM 0.3606 mL 1.8030 mL 3.6059 mL 9.0149 mL
10 mM 0.1803 mL 0.9015 mL 1.8030 mL 4.5074 mL
15 mM 0.1202 mL 0.6010 mL 1.2020 mL 3.0050 mL
DMSO 20 mM 0.0901 mL 0.4507 mL 0.9015 mL 2.2537 mL
25 mM 0.0721 mL 0.3606 mL 0.7212 mL 1.8030 mL
30 mM 0.0601 mL 0.3005 mL 0.6010 mL 1.5025 mL
40 mM 0.0451 mL 0.2254 mL 0.4507 mL 1.1269 mL
50 mM 0.0361 mL 0.1803 mL 0.3606 mL 0.9015 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PD 168368
目录号:
HY-116216
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