GR159897 - CAS:158848-32-9

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GR159897 (Synonyms:({1-[2-(5-氟-1H-吲哚-3-基)乙基]-4-甲氧基-4-哌啶基}甲基)(苯基)锍醇)

目录号 : KCM11745 CAS No. : 158848-32-9 纯度 : ≥98%

Data Sheet SDS 产品使用指南

GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK) receptor. It binds to NK receptors (K = 0.32 nM) and is selective for NK over NK and NK receptors in radioligand binding assays (Ks = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK receptor agonist GR64349 in isolated guinea pig trachea (pA = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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Other Forms of Rapamycin:

Maropitant citrate In-stock
R 396 In-stock
GR159897 In-stock
Benzomalvin C In-stock
Benzomalvin B In-stock

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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.

体外研究

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.
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.

Cell Proliferation Assay

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

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

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).

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

分子式

C₂₃H₂₇FN₂O₂S

分子量

414.54

CAS号

158848-32-9

中文名称

5-F氟-3-[2-[4-甲氧基-4-[[(r)-苯基亚磺酰基]甲基]-1-哌啶基]乙基]-1H-吲哚

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: 31 mg/mL (74.78 mM; Need ultrasonic and warming)

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
10 mM	0.2412 mL	1.2062 mL	2.4123 mL

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。

纯度： ≥98%