中文名称: LY334370
英文名称: LY334370
CAS No: 182563-08-2
分子式: C21H22FN3O
分子量: 351.42
L10029 LY334370 ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO和水(≥5mg/mL)
产品描述:

基本信息

产品编号:

L10029

产品名称:

LY334370

CAS:

182563-08-2

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C21H22FN3O

溶于液体

-80℃

两年

分子量

351.42

-20℃

1个月

化学名: 

4-fluoro-N-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]benzamide

Solubility (25°C):

 

体外:

 

DMSO

≥ 55.5 mg/mL (157.93mM)

Ethanol

 

Water

 

体内(现配现用):

1.请依序添加每种溶剂:10% DMSO→40% PEG300→ 5% Tween-80→45% saline

Solubility: ≥ 2.5 mg/mL (7.11mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (7.11mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50 μ L Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。

2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.11mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (7.11mM,饱和度未知) 的澄清溶液。以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均 匀。

3.请依序添加每种溶剂:10% DMSO→90% corn oil

Solubility: ≥ 2.5 mg/mL (7.11mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (7.11mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.8456mL

14.2280mL

28.4560mL

5mM

0.5691mL

2.8456mL

5.6912mL

10mM

0.2846mL

1.4228mL

2.8456mL

 

生物活性

产品描述

一种选择性的SR-1F激动剂。

靶点

5-HT1F Receptor 1.6nM (Ki)

体外研究

LY334370 has no vasoconstrictor effects on human cerebral arteries in vitro until a dose of 10-5 M, at which it produces a contraction of 8.5±5.7%; however, this is not significant.

体内研究

Following intravenous administration of LY334370 at 3 mg/kg (n=3) or 10 mg/kg (n=6) electrical stimulation evokes an increase in dural blood vessel diameter of 135±6% and 106±11%, respectively, which is not significantly different from the respective control values. LY334370 has no effect on dural blood vessel diameter per se, since the actualdural blood vessel diameter is 43±4 arbitrary units before drug and 43±4 arbitrary units 15 min after injection of LY334370 (10 mg/kg) .

 

推荐实验方法(仅供参考)

Cell Assay

Human cerebral artery is used in this study. Segments are prepared as previously described, but briefly they are placed in a buffer solution containing (mM) NaCl 119, NaHCo3 15, KCl 4.6, CaCl2 1.5, NaH2PO4 1.2, MgCl2 1.2, and glucose 5.5. Sections of vessel about 0.5 mm in diameter and 1 to 2 mm in length are mounted in a temperature-controlled tissue bath (37°C) containing buffer solution bubbled with 95% O2 and 5% CO2. The vessel segments are given a tension of 4 mN and allowed to stabilize at this tension for 1 to 1.5 h. Vessel reactivity is tested by exposure to 60 mM KCl. This is done twice for each segment and only if the response is similar to the segment used for LY334370 testing. Responses to LY334370 is calculated as a percentage of the maximum KC1 response.

 

Animal Administration

Male Sprague-Dawley rats (300 to 400 g) are used. Rats are placed in a stereotaxic frame, the skull exposed and thinned by drilling to reveal a branch of the middle meningeal artery whose diameter is measured continuously through the intact skull using intravital microscopy and a video dimension analyser. Neurogenic vasodilation is evoked using a bipolar stimulating electrode placed on the surface of the cranial window approximately 200 μM from the vessel of interest. A control vasodilation response to electrical stimulation is produced and 5 min later LY334370 (3 or 10 mg/kg, iv.) is given and the electrical stimulation repeated after a further 15 min. The mean maximum percentage increase in dural vessel diameter relative to pre-stimulus baseline is calculated for each response and comparisons of vasodilation responses evoked in the presence or absence of LY334370 are made by analysis of variance followed by paired t-tests.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):