ADX71743
- CAS号:1431641-29-0
- 英文名:ADX71743
- 中文名:ADX71743
- CBNumber:CB53364104
- 分子式:C17H19NO2
- 分子量:269.34
- MOL File:1431641-29-0.mol
- 沸点 :405.1±24.0 °C(Predicted)
- 密度 :1.130±0.06 g/cm3(Predicted)
- 储存条件 :-20°C
- 溶解度 :DMSO: 5mg/mL, clear (warmed)
- 酸度系数(pKa) :-0.05±0.40(Predicted)
- 形态 :powder
- 颜色 :white to beige
ADX71743性质、用途与生产工艺
- 生物活性 ADX71743 是一种高度选择性，非竞争性且透过血脑屏障的代谢型谷氨酸受体 7 负变构调节剂 (mGlu7 NAM)。ADX71743 具有抗焦虑活性。
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靶点
mGlu7
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体外研究
ADX71743 has an IC 50 of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction.
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal.
ADX71743 can against an EC 80 of glutamate (IC 50 of 22 nM) as well as against an EC 80 of L-AP4 (IC 50 of 125 nM).
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体内研究
ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T 1/2 of 0.68, 0.40 hours, a C max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Animal Model: Adult male C57Bl6/J mice (24-30 g) Dosage: 50, 100, 150 mg/kg Administration: SC Result: Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg). Animal Model: Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g) Dosage: 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis) Administration: SC Result: Had a T 1/2 of 0.68, 0.40 hours, a C max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T 1/2 of 1.5 hours, a C max of 16800 ng/ml of 100 mg/kg in rat.
- 更新日期：2024/11/08
- 产品编号：HY-110278
- 产品名称：ADX71743
- CAS编号：
- 包装：5 mg
- 价格：3383元
- 更新日期：2024/08/19
- 产品编号：HY-110278
- 产品名称：ADX71743
- CAS编号：
- 包装：10 mg
- 价格：5416元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32161
- 优势度：58
- 公司名称：BOC Sciences
- 联系电话：--
- 电子邮件：info@bocsci.com
- 国家：美国
- 产品数：0
- 优势度：65
- 公司名称：TargetMol Chemicals Inc.
- 联系电话： +8613564774135
- 电子邮件：zijue.cai@tsbiochem.com
- 国家：美国
- 产品数：19881
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
