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

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.

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GR 159897

GR 159897 構造式

CAS 番号 : 158848-32-9

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5 mg $308 在庫あり
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GR 159897 関連抗体

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Neurokinin Receptor アイソフォーム固有の製品をすべて表示:

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NK1R NK2R NK3R

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製品説明

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]

NK2R

10 (pKi, Rat colon membrane)

hNK2

9.51 (pKi, CHO cell)

体外実験

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].

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

GR 159897 関連抗体

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.
体内実験

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].

MedChemExpress (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

分子式

C23H27FN2O2S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=[S@](CC1(OC)CCN(CCC2=CNC3=C2C=C(F)C=C3)CC1)C4=CC=CC=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, sealed storage, away from moisture

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

DMSO : 31 mg/mL (74.78 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2412 mL 1.2062 mL 2.4123 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.6%

COA (256 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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GR 159897 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
GR 159897
製品番号:
HY-107691
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