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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -Mirogabalin
Mirogabalin

Chemical Structure : Mirogabalin

CAS No.: 1138245-13-2

Mirogabalin (DS-5565;DS5565)

货号: PC-43138Not For Human Use, Lab Use Only.

Mirogabalin (DS-5565) is a potent, selective ligand of the α2δ subunit of voltage-gated calcium channels with Kd of 13.5/22.7/27.0/47.6 nM for huamn α2δ-1, human α2δ-2, rat α2δ-1 and rat α2δ-2 subunits, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Mirogabalin (DS-5565) is a potent, selective ligand of the α2δ subunit of voltage-gated calcium channels with Kd of 13.5/22.7/27.0/47.6 nM for huamn α2δ-1, human α2δ-2, rat α2δ-1 and rat α2δ-2 subunits, respectively.
Mirogabalin (DS-5565) exhibits a slower dissociation rate for the α2δ-1 subunit than the α2δ-2 subunit compared to pregabalin.
Mirogabalin (DS-5565) shows more potent and longer lasting analgesic effects in experimental neuropathic pain models, partial sciatic nerve ligation rats and streptozotocin-induced diabetic rats.
Mirogabalin (DS-5565) inhibits rota-rod performance and locomotor activity in rats.

物理化学性质&存储条件

分子量 209.2848
分子式 C12H19NO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 10 mM; Methanol: ≥ 35 mg/mL

Chemical Name/SMILES

Bicyclo[3.2.0]hept-3-ene-6-acetic acid, 6-(aminomethyl)-3-ethyl-, (1R,5S,6S)-

参考文献

1. Merante D, et al. Pain Med. 2017 Nov 1;18(11):2198-2207.

2. Vinik A, et al. Diabetes Care. 2014 Dec;37(12):3253-61.

3. Domon Y, et al. J Pharmacol Exp Ther. 2018 Mar 21. pii: jpet.117.247551.

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