- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: Vernakalant (Hydrochloride)
- Price: ￥6076.0/25mg ￥2246.0/5mg ￥14606.0/100mg ￥9106.0/50mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Vernakalant (Hydrochloride)
- Price: $750.0/100mg $1500.0/250mg $3000.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Henan Tianfu Chemical Co., Ltd.
- China
- Product Name: VERNAKALANT HYDROCHLORIDE
- Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Anson
748810-28-8
748810-28-8 structure
- Name: Vernakalant (Hydrochloride)
- Chemical Name: (3R)-1-{(1R,2R)-2-[2-(3,4-Dimethoxyphenyl)ethoxy]cyclohexyl}-3-py rrolidinol hydrochloride (1:1)
- CAS Number: 748810-28-8
- Molecular Formula: C20H32ClNO4
- Molecular Weight: 385.92500
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
- Create Date: 2018-03-06 08:00:00
- Modify Date: 2024-01-28 07:33:48
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Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively.
| Name | (3R)-1-{(1R,2R)-2-[2-(3,4-Dimethoxyphenyl)ethoxy]cyclohexyl}-3-py rrolidinol hydrochloride (1:1) |
|---|---|
| Synonyms |
Vernakalant Hydrochloride
Vernakalant (Hydrochloride) |
| Description | Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na+ and atria-preferred K+ channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channelwt, Kv1.5 channelI508F, Kv1.5 channelT479A, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 13.35±0.93 μM (Kv1.5 channelwt), 0.61±0.03 μM (I508F), 1.63±0.09 μM (Kv1.5 channel T479A)[1] |
| In Vitro | Block of Kv1.5 by Vernakalant Hydrochloride is mediated after channel activation, because Vernakalant causes a relatively rapid onset of block of channel current upon depolarization but little evidence of resting or “tonic” block of the channel. In the presence of 10 μM Vernakalant, rapid block is apparent after channel opening, and a steady-state current level is rapidly reached. The most important effect is the reduction in potency for Vernakalant centered at I502A, which had an IC50 of 329±19 μM (n=4-10), compared with a control IC50 of 13.4±0.9 μM (n=5-23), which is a 25-fold decrease in potency. V505A, I508A, T480A, and C500A showed lesser reductions in potency on Kv1.5, of between 3- and 4-fold. I508Y in our experiments increased the IC50 for Vernakalant on Kv1.5 to 24.7 μM, again similar to the reported value for hERG[1]. |
| References |
| Molecular Formula | C20H32ClNO4 |
|---|---|
| Molecular Weight | 385.92500 |
| Exact Mass | 385.20200 |
| PSA | 51.16000 |
| LogP | 3.38060 |
| Storage condition | 2-8℃ |