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:等待报价

产品详情

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.

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