2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. GR 159897

GR 159897 是一种高效，选择性，竞争性，可通过血脑屏障的非肽神经激肽 2 (NK2) 受体拮抗剂。GR 159897 对 NK1 和 NK3 受体几乎没有亲和力。GR 159897 抑制 [3H]GR100679 与人 NK2-CHO 细胞和大鼠结肠膜的结合，pKi 值分别为 9.51 和 10。拮抗支气管收缩。抗焦虑和抗肿瘤作用。

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GR 159897 Chemical Structure

GR 159897 Chemical Structure

CAS No. : 158848-32-9

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规格 价格 是否有货 数量
10 mg ￥6048
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Customer Review

GR 159897 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects[1][2].

IC50 & Target[1]

NK2

10 (pKi, Rat colon membrane)

hNK2

9.51 (pKi, CHO cell)

体外研究
(In Vitro)

GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells[2].
GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM and 4T1 cells) treatment increases phosphorylation of P38, while inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM and 4THM but not in 4T1 cells[2].

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

GR 159897 相关抗体:

Cell Proliferation Assay[2]

Cell Line: 4T1, 4THM, 4TLM and 67NR cells
Concentration: 10 μM, 30 μM
Incubation Time: 72 hours
Result: Inhibited proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells.

Western Blot Analysis[2]

Cell Line: 4TBM, 4TLM, 4THM and 4T1 cells
Concentration: 10 μM, 30 μM
Incubation Time: 40 hours
Result: Increased phosphorylation of P38.
体内研究
(In Vivo)

GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h)[1].

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

Animal Model: Guinea-pigs[1]
Dosage: 0.12 mg/kg
Administration: Intravenous injection
Result: Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
分子量

414.54

Formula

C23H27FN2O2S
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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 31 mg/mL (74.78 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4123 mL 12.0616 mL 24.1231 mL
5 mM 0.4825 mL 2.4123 mL 4.8246 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 (sealed storage, away from moisture)。-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

只
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
参考文献

GR 159897 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 (sealed storage, away from moisture)。-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
DMSO 1 mM 2.4123 mL 12.0616 mL 24.1231 mL 60.3078 mL
5 mM 0.4825 mL 2.4123 mL 4.8246 mL 12.0616 mL
10 mM 0.2412 mL 1.2062 mL 2.4123 mL 6.0308 mL
15 mM 0.1608 mL 0.8041 mL 1.6082 mL 4.0205 mL
20 mM 0.1206 mL 0.6031 mL 1.2062 mL 3.0154 mL
25 mM 0.0965 mL 0.4825 mL 0.9649 mL 2.4123 mL
30 mM 0.0804 mL 0.4021 mL 0.8041 mL 2.0103 mL
40 mM 0.0603 mL 0.3015 mL 0.6031 mL 1.5077 mL
50 mM 0.0482 mL 0.2412 mL 0.4825 mL 1.2062 mL
60 mM 0.0402 mL 0.2010 mL 0.4021 mL 1.0051 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.

Keywords:

GR 159897158848-32-9GR159897GR-159897Neurokinin ReceptorNK receptorTachykinin receptorGR 64349non-peptidedurationbronchoconstrictiontachykininNK2anxiolytic-likeCNSP38anti-tumorInhibitorinhibitorinhibit

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