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Merck

SML0385

Sigma-Aldrich

ML218

≥98% (HPLC)

別名:

3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]benzamide, CID 45115620, VU0413807, VU0424199-1

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About This Item

実験式(ヒル表記法):
C19H26Cl2N2O
CAS番号:
分子量:
369.33
UNSPSCコード:
12352200
PubChem Substance ID:
NACRES:
NA.77

品質水準

アッセイ

≥98% (HPLC)

フォーム

powder

white to beige

溶解性

DMSO: 10 mg/mL (clear solution)

保管温度

2-8°C

SMILES記法

CC(C)(C)CCN1C[C@H]2C(CNC(=O)c3cc(Cl)cc(Cl)c3)[C@H]2C1

InChI

1S/C19H26Cl2N2O/c1-19(2,3)4-5-23-10-16-15(17(16)11-23)9-22-18(24)12-6-13(20)8-14(21)7-12/h6-8,15-17H,4-5,9-11H2,1-3H3,(H,22,24)/t15-,16-,17+

InChI Key

GSJIGYLGKSBYBC-OSYLJGHBSA-N

アプリケーション

ML218 has been used as a:
  • T-type channel blocker to test its effect on the nociceptive behavior associated with homocysteinemia rats
  • T-type voltage-sensitive calcium channel (VSCC) inhibitor in osteoblasts
  • T-type calcium channel blocker to test its effect on the viability of neural progenitor cells

生物化学的/生理学的作用

ML218 (CID 45115620) is a potent and selective T-Type (Cav3.1, Cav3.2, Cav3.3) calcium channel inhibitor (Cav3.2, IC50 = 150 nM in Ca2+ flux; Cav3.2 IC50 = 310 nM and Cav3.3 IC50 = 270 nM with good Drug metabolism/Pharmacokinetics. In a panel of 68 GPCRs, ion channels and transporters, ML218 was found to bind significantly only two other targets (sodium channel site 2 and sigma 1) and had no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. It showed robust inhibition of calcium current in STN neurons and was orally active in a rodent model of Parkinson′s Disease.
ML218 is a potent, selective T-Type calcium channel inhibitor.

特徴および利点

This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML0385-VAR:
SML0385-25MG:
SML0385-BULK:
SML0385-5MG:
SML0385-IP:


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以前この製品を購入いただいたことがある場合

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文書ライブラリにアクセスする

Brittany D Spitznagel et al.
ACS chemical neuroscience, 11(21), 3658-3671 (2020-11-05)
Malignant migrating partial seizures of infancy is a rare, devastating form of epilepsy most commonly associated with gain-of-function mutations in the potassium channel, Slack. Not only is this condition almost completely pharmacoresistant, there are not even selective drug-like tools available
Retsu Mitsui et al.
Pflugers Archiv : European journal of physiology, 468(2), 279-291 (2015-11-05)
Postcapillary venules (PCVs) play a critical role in regulating capillary hydrostatic pressure, but their contractile mechanisms are not well understood. We examined the properties of spontaneous vasomotion and corresponding Ca(2+) transients in gastric PCV. In the rat gastric submucosa, changes
Andreas Feigenspan et al.
Experimental eye research, 195, 108028-108028 (2020-04-12)
Expression patterns of voltage-gated ion channels determine the spatio-temporal dynamics of ion currents that supply excitable neurons in developing tissue with proper electrophysiological properties. The purpose of the study was to identify fast cationic inward currents in mouse retinal horizontal
Kaori Sato-Numata et al.
The journal of physiological sciences : JPS, 70(1), 49-49 (2020-10-17)
Arginine vasopressin (AVP) neurons play essential roles in sensing the change in systemic osmolarity and regulating AVP release from their neuronal terminals to maintain the plasma osmolarity. AVP exocytosis depends on the Ca2+ entry via voltage-gated Ca2+ channels (VGCCs) in
Nicholas Mikolajewicz et al.
eLife, 7 (2018-10-17)
Bone cells sense and actively adapt to physical perturbations to prevent critical damage. ATP release is among the earliest cellular responses to mechanical stimulation. Mechanical stimulation of a single murine osteoblast led to the release of 70 ± 24 amole

資料

We offers many products related to calcium channels for your research needs.

We offers many products related to calcium channels for your research needs.

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