GR159897 - CAS:158848-32-9

您当前的位置：

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

加入购物车大包装询价

Other Forms of Rapamycin:

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

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

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.

IC₅₀&Target

NK2R hNK2

10 (pKi, Rat colon membrane) 9.51 (pKi, CHO cell)

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%

Data Sheet

SDS

产品使用指南

Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器