1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. PTAC oxalate

PTAC oxalate 是一种选择性毒蕈碱受体 (muscarinic receptor) 配体。PTAC oxalate 是 M2 和 M4 的部分激动剂,是 M1、M3 和 M5 的拮抗剂,对于 CHO 细胞中的 hM1-5,Ki 值为 0.2-2.8 nM。PTAC oxalate 减轻神经性疼痛的机械异常性疼痛并具有抗抑郁作用。

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PTAC oxalate Chemical Structure

PTAC oxalate Chemical Structure

CAS No. : 201939-40-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects[1][2].

IC50 & Target[1][2]

mAChR1

0.6 nM (Ki)

mAChR2

2.8 nM (Ki)

mAChR3

0.2 nM (Ki)

mAChR4

0.2 nM (Ki)

mAChR5

0.8 nM (Ki)

体内研究
(In Vivo)

PTAC oxalate (0.01, 0.05 mg/kg; 腹腔给药) 在 0.05 mg/kg 时可以减轻机械异常性疼痛。PTAC oxalate 在 0.05 mg/kg 剂量下可缩短假手术组和神经损伤组小鼠的不动时间,但在 0.01 mg/kg 剂量下则不会[2]

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

Animal Model: Mouse model of neuropathic pain[2]
Dosage: 0.01, 0.05 mg/kg
Administration: IP
Result: The mechanical allodynia was alleviated with 0.05 mg/kg.
At 0.05 mg/kg increased the paw withdrawal thresholds (PWTs) of the nerve-injury groups injected at day 4 after nerve injury.
At 0.01 mg/kg had no effect on the PWTs in the sham and nerve-injury groups injected at day 14 after nerve injury.
分子量

359.46

Formula

C14H21N3O4S2

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

PTAC oxalate 相关分类

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  • 稀释计算器

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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.

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产品名称:
PTAC oxalate
目录号:
HY-107656
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