Vatinoxan hydrochloride (MK-467 hydrochloride)
(Synonyms: MK-467 hydrochloride; L-659066 hydrochloride) 目录号 : GC30938
Vatinoxan hydrochloride (MK-467 hydrochloride) (MK-467 hydrochloride;L-659066 hydrochloride) 是一种外周 α2 肾上腺素能受体拮抗剂。
Cas No.:130466-38-5
Sample solution is provided at 25 µL, 10mM.
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Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.
Vatinoxan alone increases cardiac index and tissue oxygen delivery and has no deleterious adverse effects. Vatinoxan attenuates or prevents dexmedetomidine’s systemic hemodynamic effects in a dose-dependent manner when given simultaneously i.v. but has no effect on the pulmonary outcome in conscious dogs. A 50:1 dose ratio (Vatinoxan:dexmedetomidine) induces the least alterations in cardiovascular function[1]. Vatinoxan dose-dependently attenuates the bradycardia associated with dexmedetomidine, and shortens the sedative effect without altering its quality. Vatinoxan may be useful in attenuating reductions in heart rate in conscious catsadministered dexmedetomidine[2].
[1]. Honkavaara JM, et al. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7. [2]. Honkavaara J, et al. The effect of MK-467, a peripheral α2-adrenoceptor antagonist, on dexmedetomidine-inducedsedation and bradycardia after intravenous administration in conscious cats. Vet Anaesth Analg. 2017 Feb 22. pii: S1467-2987(16)31387-3.
Animal experiment: | Dogs[1]Eight dogs receive either dexmedetomidine (10 μg/kg), Vatinoxan (250 μg/kg or dexmedetomidine (10 μg/kg) with increasing doses of Vatinoxan (250 μg/kg, 500 μg/kg and 750 μg/kg). Treatments are given intravenously (i.v.) in a randomized, crossover design with a 14-day ishout period. Systemic hemodynamics and arterial blood gas analyses are recorded at baseline and at intervals up to 90 min after drugs administration[1].Cats[2]Cats are administered seven IV treatments are administered at least 2 weeks apart, consisting of dexmedetomidine 12.5 μg/kg (D12.5) and 25 μg/kg (D25), Vatinoxan 300 μg/kg (M300), and D25 combined with 75, 150, 300 and 600 μg/kg of Vatinoxan (D25M 75, D25M150, D25M300 and D25M600, respectively). Heart rates (HR) are recorded via telemetry and sedation assessed with a simple descriptive score and a visual analogue scale prior to treatments and at intervals until 8 hours thereafter[2]. |
References: [1]. Honkavaara JM, et al. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7. | |
| Cas No. | 130466-38-5 | SDF | |
| 别名 | MK-467 hydrochloride; L-659066 hydrochloride | ||
| 化学名 | N-(2-((2R,12bS)-2'-oxo-1,3,4,6,7,12b-hexahydrospiro[benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl)ethyl)methanesulfonamide hydrochloride | ||
| Canonical SMILES | [H]Cl.CS(=O)(NCCN([C@]1(CN2)CCN3CCC4=C(OC5=CC=CC=C54)[C@]3([H])C1)C2=O)=O | ||
| 分子式 | C20H27ClN4O4S | 分子量 | 454.97 |
| 溶解度 | Water : ≥ 133 mg/mL (292.33 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1979 mL | 10.9897 mL | 21.9795 mL |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3959 mL |
| 10 mM | 0.2198 mL | 1.099 mL | 2.1979 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet