PTAC oxalate

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PTAC oxalate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

201939-40-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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、hM2、hM3、hM4 和 hM5，K_i值分别为 0.6、2.8、0.2、0.2 和 0.8 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。

生物活性

PTAC oxalate is a selectivemuscarinic receptorligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (K_ivalues of 0.6, 2.8, 0.2, 0.2 and 0.8 nM for hM1, hM2, hM3, hM4 and hM5 in CHO cells, respectively). 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) 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]。

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

201939-40-4

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.