|1-((3-(4-氯苯乙基)-1,2,4-恶二唑-5-基)甲基)-7-甲基-1H-嘌呤-6(7H)-酮|CsnPharm

CAS No.: 1883711-97-4

AM-0902 Catalog No. CSN21376

Synonyms: 1-((3-(4-Chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1H-purin-6(7H)-one

Potent and selective TRPA1 antagonist (IC50 = 0.02 μM for human TRPA1). Exhibits no siginificant activity against human TRPV1 or TRPV4, and rat TRPV1, TRPV3 or TRPM8. Exhibits efficacy in a rat pain model. Orally bioavailable.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TRPA1, a nonselective cation channel and member of the transient receptor potential (TRP) superfamily of ion channels, is highly expressed in sensory neurons of the dorsal root ganglia and is activated by a range of irritants. AM-0902 is a potent and selective TRPA1 antagonist with IC50 values of 0.02μM and 0.024μM for hTRPA1 and rTRPA1, respectively. AM-0902 could inhibit Ca²⁺ entering the cell upon activation and opening of the channel with AITC with IC50 value of 0.131μM and 0.071μM for hTRPA1 and rTRPA1, respectively. Oral pre-treatment with AM-0902 at dose of 10mg/kg and 30mg/kg 1h before injection of AITC (0.1%) significantly reduced the AITC flinching in rats. Application of AM-0902 significantly attenuated the elevated frequency of spontaneous EPSCs and miniature EPSCs, the amplitude of monosynaptic EPSCs evoked from the dorsal root in lamina I neurons of CFA-treated rats without effect on evoked or miniature EPSCs in lamina I neurons of vehicle-treated rats. Also, intrathecal injection of AM-0902 significantly reduced pain hypersensitivity in CFA-treated rats without effect on acute nociception in vehicle-treated rats.

动物研究

剂量

Mice: 30 mg/kg^[1] (p.o.) Rat: 0.5 mg/kg^[2] (i.v.); 30 mg/kg^[2] (p.o.), 0.3 mg/kg - 300 mg/kg^[3] (p.o.)

给药途径

p.o., i.v.

动物药代数据

Animal	Rats^[2]
Dose	0.5 mg/kg (i.v.) 30 mg/kg (p.o.)
Administration	i.v. p.o.
F	60% (p.o.)
AUC_inf	19.8 μM·h (p.o.)
T_1/2	0.6 h (i.v.) 2.8 h (p.o.)
T_max	0.8 h (p.o.)
CL	2.5 L/h/kg (i.v.)
C_max	7.5 μM (p.o.)
CL_u	9 (i.v.)
Vss	1.7 L/kg (i.v.)

参考文献

[1] Takahashi N, Chen HY, et al. Cancer Cells Co-opt the Neuronal Redox-Sensing Channel TRPA1 to Promote Oxidative-Stress Tolerance. Cancer Cell. 2018 Jun 11;33(6):985-1003.e7.
[2] Schenkel LB, Olivieri PR, et al. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809.
[3] Lehto SG, Weyer AD, et al. Selective antagonism of TRPA1 produces limited efficacy in models of inflammatory- and neuropathic-induced mechanical hypersensitivity in rats. Mol Pain. 2016 Nov 29;12. pii: 1744806916677761. Print 2016.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6969 mL
- 13.4846 mL
- 26.9692 mL
- 5 mM
- 0.5394 mL
- 2.6969 mL
- 5.3938 mL
- 10 mM
- 0.2697 mL
- 1.3485 mL
- 2.6969 mL

技术信息

CAS号

1883711-97-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15ClN6O2

运输

蓝冰

分子量

370.79

别名

1-((3-(4-Chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1H-purin-6(7H)-one

溶解度

DMSO	150.0 mg/mL (404.5 mM)

动物实验配方

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AM-0902 Catalog No. CSN21376

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