2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. JNJ16259685

JNJ16259685 是一种选择性的 mGlu1 receptor 拮抗剂，能够浓度依赖性地抑制 mGlu1 的突触的活化，IC50 值为 19 nM。

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JNJ16259685 Chemical Structure

JNJ16259685 Chemical Structure

CAS No. : 409345-29-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1089
In-stock
1 mg ￥396
In-stock
5 mg ￥990
In-stock
10 mg ￥1600
In-stock
25 mg ￥3300
In-stock
50 mg ￥5500
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

JNJ16259685 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 mGluR 亚型特异性产品:

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.

IC50 & Target[4]

mGluR1

19 nM (IC50)

体外研究
(In Vitro)

JNJ16259685 potently and completely inhibits the glutamate (30 μM)-induced increase in intracellular Ca2+ concentrations at the rat mGlu1a receptor with an IC50 value of 3.24±1.00 nM. IC50 values for CPCCOEt and BAY 36-7620 are 17.8±10.3 μM and 161±38 nM, respectively. The potency of JNJ16259685 in blocking glutamate (30 μM)-induced Ca2+ mobilization at the human mGlu1a receptor is 1.21±0.53 nM (IC50 n=3). JNJ16259685 inhibits the glutamate (3 μM)-induced rise in intracellular Ca2+ concentrations at the rat mGlu5a receptor with an IC50 value of 1.31±0.39 μM (n=4). JNJ16259685 blocks glutamate (3 μM)-induced Ca2+ mobilization at the human mGlu5 receptor with an IC50 of 28.3±11.7 μM (n=4). JNJ16259685 does not exhibit agonist activity at any of the group I mGlu receptors[3].

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

JNJ16259685 相关抗体:
体内研究
(In Vivo)

JNJ16259685 (0.125, 0.25, 0.5, 1, 2, 4 and 8 mg/kg, i.p) significantly reduces the time spent in digging behaviours (0.25-8 mg/kg), threat (all doses) and attack, in comparison with vehicle group[1]. JNJ16259685 (30 mg/kg) produces very minimal effects on locomotor activity. JNJ16259685 dramatically reduces rearing behavior, exploration of a novel environment and lever pressing for a food reward (rat: 0.3 mg/kg; mouse: 1 mg/kg). Subcutaneously administered JNJ16259685 (30 mg/kg) has no effect on reflexive startle responses to loud auditory stimuli or foot shock in mice[2]. JNJ16259685 exhibits high potencies in occupying central mGlu1 receptors in the rat cerebellum and thalamus (ED50=0.040 and 0.014 mg/kg, respectively)[3].

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

325.40

Formula

C20H23NO3
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (307.31 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0731 mL 15.3657 mL 30.7314 mL
5 mM 0.6146 mL 3.0731 mL 6.1463 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (8.45 mM); 澄清溶液

    此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.75 mg/mL (8.45 mM); 澄清溶液

    此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Animal Administration
[1][2]

Mice[1]
Nine groups of mice are used. Animals are randomLy allocated to two control groups (n=15 each) receiving only saline or saline (90%) plus DMSO (10%), and seven experimental groups (N=14-16 each) receiving JNJ16259685 injections. JNJ16259685 is diluted in saline (90%) plus DMSO (10%) to provide appropriate doses for injections and administered in seven doses: 0.125, 0.25, 0.5, 1, 2, 4 and 8 mg/kg. The doses are chosen on the basis of recent behavioural studies using this compound. Drug or vehicle is injected intraperitoneally in a volume of 10 mL/kg.
Rats[2]
This procedure is used to measure overt behavioral, neurological and autonomic responses to the drug challenge. Briefly, rats are randomLy separated into four groups (n=6), each of which receives a different dose (0, 3, 10, or 30 mg/kg) of JNJ16259685. An expert observer, blind to the drug treatment of the animals, assesses and scores the animals at 30, 60, 120, and 240 min post-injection. The animals are assessed for passivity, body elevation, limb position, limb tone, body tone, gait, and pupil size. For each of these behaviors, a score of 0 is assigned to animals that appeared “normal”, whereas scores of±1,±2, or±3 indicated mild, moderate, or severe increases (+) or decreases (−) from normality. Individual animals that receive a score of±2, or greater, are considered to be significantly effected on the measure. A dose is considered to have a significant effect if 3 or more of the animals receive a score of greater than±2.

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

JNJ16259685 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0731 mL 15.3657 mL 30.7314 mL 76.8285 mL
5 mM 0.6146 mL 3.0731 mL 6.1463 mL 15.3657 mL
10 mM 0.3073 mL 1.5366 mL 3.0731 mL 7.6829 mL
15 mM 0.2049 mL 1.0244 mL 2.0488 mL 5.1219 mL
20 mM 0.1537 mL 0.7683 mL 1.5366 mL 3.8414 mL
25 mM 0.1229 mL 0.6146 mL 1.2293 mL 3.0731 mL
30 mM 0.1024 mL 0.5122 mL 1.0244 mL 2.5610 mL
40 mM 0.0768 mL 0.3841 mL 0.7683 mL 1.9207 mL
50 mM 0.0615 mL 0.3073 mL 0.6146 mL 1.5366 mL
60 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2805 mL
80 mM 0.0384 mL 0.1921 mL 0.3841 mL 0.9604 mL
100 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7683 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:

JNJ16259685409345-29-5JNJ 16259685JNJ-16259685mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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