JNJ-40411813（ADX 71149）_CAS:1127498-03-6

产品属性

CAS号：1127498-03-6

重量（克）：1g,10g

价格（元）：询价

时间：2020-09-22 10:20:56

交易状态：等待担保

产品信息

98%+，接受定制

Description

JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.

IC₅₀ & Target^[1]

mGlu2 Receptor

147 nM (EC₅₀)

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01932320	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	February 2010	Phase 1
NCT01323205	Janssen Research & Development, LLC	Schizophrenia	May 2011	Phase 2
NCT01932333	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	May 2010	Phase 1

Molecular Weight

344.88

Formula

C₂₀H₂₅ClN₂O

CAS No.

1127498-03-6

SMILES

O=C1C(Cl)=C(N2CCC(C3=CC=CC=C3)CC2)C=CN1CCCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (72.49 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8996 mL	14.4978 mL	28.9956 mL
5 mM	0.5799 mL	2.8996 mL	5.7991 mL
10 mM	0.2900 mL	1.4498 mL	2.8996 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。-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。

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

1.

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

Solubility: 2.5 mg/mL (7.25 mM); Suspended solution; Need ultrasonic and warming
2.

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

Solubility: ≥ 2.5 mg/mL (7.25 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: 2.5 mg/mL (7.25 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 MCE 网站选购。

References

[1]. Cid JM, et al. Discovery of 1-Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor. J Med Chem. 2014 Aug 14;57(15):6495-512.