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Mirogabalin {[allProObj[0].p_purity_real_show]}

货号：A181027 同义名： DS5565

Mirogabalin是一种优先选择性的 α2δ-1 配体，具有高效能和对中枢神经系统电压敏感钙通道复合体中 α2δ-1 亚单位的高度选择性。

Mirogabalin 化学结构 CAS号：1138245-13-2
Mirogabalin 化学结构
CAS号：1138245-13-2
Mirogabalin 3D分子结构
CAS号：1138245-13-2
Mirogabalin 化学结构 CAS号：1138245-13-2
Mirogabalin 3D分子结构 CAS号：1138245-13-2
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Mirogabalin 纯度/质量文件 产品仅供科研

货号：A181027 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt 99%+
Clevidipine ✔ 97%
Verapamil HCl ✔ 99%
Amlodipine ✔ 99%
Amlodipine maleate ✔ 98%
(+)-cis-Diltiazem HCl ✔ 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		99%+
Tanshinone IIA sulfonate sodium ✔ 98%
Ulixacaltamide ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		ERK,p38 MAPK,ROS 99%+
Fasudil HCl ✔ PKA,Rho 98%
ML-9 ✔ MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 99%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 99%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 99%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

 		98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 99%
Cinepazide Maleate ✔ 99% (HPLC)
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Ranolazine ✔ 98%
Praeruptorin A ✔ p38 MAPK,Akt 98%
Ranolazine 2HCl ✔ 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		98%
Levamlodipine besylate ✔ 97%
Carboxyamidotriazole Orotate ✔ 98%
IGS-1.76 ✔ 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mirogabalin 生物活性

描述 Mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels, is being developed to treat pain associated with diabetic peripheral neuropathy and postherpetic neuralgia. Mirogabalin shows potent and selective binding affinities for the human and rat α2δ subunits, and slower dissociation rates for the α2δ-1 subunit than the α2δ-2 subunit. It shows potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for side effects of the central nervous system[3]. In rats subjected to spinal cord injury, mechanical allodynia was demonstrated by a decreased paw withdrawal threshold. A single oral administration of mirogabalin (2.5, 5, or 10 mg/kg) significantly increased the paw withdrawal threshold. The effects of mirogabalin were still significant 6 or 8 h after administration. The paw withdrawal threshold AUC was significantly higher in the treated animals than in the control group[4]. Mirogabalin relieved DPNP (diabetic peripheral neuropathic pain) in a dose-dependent manner; mirogabalin 30 mg/day showed statistically significant pain relief (vs placebo) in Asian DPNP patients. All doses of mirogabalin tested were well tolerated[5]. The most frequent treatment-emergent adverse events (TEAEs)-dizziness and somnolence-were expected based on mirogabalin's mechanism of action. After oral administration, mirogabalin was rapidly absorbed (time to maximum concentration, ∼1 hour) and eliminated through urine unchanged (61%-72% urinary excretion)[6].

Mirogabalin 参考文献

[1]Hutmacher MM, Frame B, et al. Exposure-response modeling of average daily pain score, and dizziness and somnolence, for mirogabalin (DS-5565) in patients with diabetic peripheral neuropathic pain. J Clin Pharmacol. 2016 Jan;56(1):67-77.

[2]Vinik A, Rosenstock J, et al; DS5565-A-U201 US Phase II Study Investigators. Efficacy and safety of mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study. Diabetes Care. 2014 Dec;37(12):3253-61.

[3]Domon Y, Arakawa N, Inoue T, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α2δ Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018;365(3):573‐582

[4]Domon Y, Kitano Y, Makino M. Analgesic effects of the novel α₂δ ligand mirogabalin in a rat model of spinal cord injury. Pharmazie. 2018;73(11):659‐661

[5]Baba M, Matsui N, Kuroha M, Wasaki Y, Ohwada S. Mirogabalin for the treatment of diabetic peripheral neuropathic pain: A randomized, double-blind, placebo-controlled phase III study in Asian patients. J Diabetes Investig. 2019;10(5):1299‐1306

[6]Brown K, Mendell J, Ohwada S, et al. Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects: Results from phase 1 studies. Pharmacol Res Perspect. 2018;6(5):e00418.

Mirogabalin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.78mL

0.96mL

0.48mL

23.89mL

4.78mL

2.39mL

47.78mL

9.56mL

4.78mL

Mirogabalin 技术信息

CAS号1138245-13-2
分子式C12H19NO2
分子量 209.285
别名 DS5565
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
溶解方案

H2O: 7.5 mg/mL(35.84 mM)，配合低频超声助溶
动物实验配方

Tags: Mirogabalin | 1138245-13-2 | DS5565 | DS 5565 | DS-5565 | Calcium Channel Inhibitor | Membrane Transporter/Ion Channel | Neuronal Signaling | Calcium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Mirogabalin 纯度/质量文件 | Mirogabalin 亚型比较 | Mirogabalin 生物活性 | Mirogabalin 参考文献 | Mirogabalin 实验方案 | Mirogabalin 技术信息

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