2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. RO5126946

RO5126946 是一种选择性、口服有效的 α7 nAChR 变构增强剂 (EC50=0.06 μM (hα7 nAChR) 和 770 nM (α7 nAChR))，能穿透血脑屏障。RO5126946 通过增大峰值电流、延缓电流衰减以及增加自发性抑制性突触后电流频率来增强突触传递和正向调控 GABA 能反应，且不影响受体从脱敏状态恢复。RO5126946 不仅能增强阈下尼古丁效应和改善联想学习，还不会干扰尼古丁原有的促认知作用。RO5126946 可用于研究阿尔茨海默病、精神分裂症等疾病相关认知障碍。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

RO5126946

RO5126946 Chemical Structure

CAS No. : 1137233-79-4

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

RO5126946 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia[1].

体外研究
(In Vitro)

RO5126946 (0.01-3 μM) 可通过 α7 nAChR 依赖的机制强效增强培养大鼠海马神经元中尼古丁诱发的电流，其 EC50 为 7.7 × 10-7 M，最大增强幅度为 2800%，且该效应不依赖于谷氨酸或 GABAₐ受体的活性[1]。
RO5126946 (0.3-1 μM) 无法在培养的大鼠海马神经元中重新激活完全脱敏的 α7 nAChR[1]。
RO5126946 (0.3 μM; ~5 min) 可增强尼古丁诱导的培养大鼠海马神经元自发放抑制性突触后电流频率升高，该效应依赖于动作电位的传导[1]。

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

RO5126946 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: rat hippocampal neurons
Concentration: 0.3-1 μM
Incubation Time: /
Result: Couldn't reactivate fully desensitized α7 nAChRs in cultured rat hippocampal neurons.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC Bioavailability
Rat[1] 3 mg/kg i.v. 3490 ± 1414 ng/mL / 4.90 h 11,600 ng·h/mL /
Rat[1] 1 mg/kg p.o. 214 ± 81 ng/mL 2.5 h 5.19 h 2280 ng·h/mL ~100 %
Rat[1] 3 mg/kg p.o. 1050 ± 31 ng/mL 4.67 h 4.00 h 11,800 ng·h/mL ~100 %
Rat[1] 10 mg/kg p.o. 3470 ± 357 ng/mL 3.33 h 2.61 h 25,900 ng·h/mL ~100 %
体内研究
(In Vivo)

RO5126946 (3-30 mg/kg；灌胃；训练前 60 分钟；单次 ) 可逆转 Scopolamine (HY-N0296) 诱导的大鼠联想记忆缺陷[1]。
RO5126946 (1 mg/kg；灌胃；训练前 60 分钟单次给药) 可增强阈下剂量尼古丁的促认知作用，从而逆转 Scopolamine 诱导的大鼠联想记忆损伤[1]。
RO5126946 (3 mg/kg，灌胃；训练前 60 分钟给药) 可逆转 Scopolamine 诱导的大鼠联想记忆障碍，且不会干扰有效剂量尼古丁的促认知作用[1]。

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

Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose 60 minutes before training
Result: Significantly reversed scopolamine-induced deficits in freezing behavior.
Resulted in a freezing percentage significantly different from both vehicle and scopolamine groups at 3 mg/kg.
Restored freezing to levels statistically indistinguishable from vehicle-treated rats at 10 and 30 mg/kg.
Showed mean pre-tone freezing <4% across all groups.
Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose 60 minutes before training
Result: Did not reverse scopolamine-induced memory deficits when administered alone.
Produced a significant reversal of scopolamine-induced memory deficits when coadministered with a subthreshold dose of nicotine.
Showed mean pre-tone freezing <2% across all groups.
Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose 60 minutes before training
Result: Significantly reversed scopolamine-induced memory deficits when administered alone.
Maintained procognitive effect when coadministered with an effective dose of nicotine.
Showed mean pre-tone freezing <3% across all groups.
分子量

408.90

Formula

C19H21ClN2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RO5126946 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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:

RO51269461137233-79-4RO 5126946RO-5126946nAChRNicotinic acetylcholine receptorsspontaneous inhibitory postsynaptic currentHEK293 cellsrat hippocampal neurons5-hydroxytryptamine 3 receptorsXenopus oocytesGABAergic responsesInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
RO5126946
目录号：
HY-124057
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z