Vatinoxan hydrochloride (MK-467 hydrochloride)

目录号: GC30938纯度: >99.50%同义词: MK-467 hydrochloride; L-659066 hydrochloride
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。

Vatinoxan hydrochloride (MK-467 hydrochloride)
Cas No.: 130466-38-5
规格价格库存数量操作
1mg¥2,448.00现货
1
10mM (in 1mL DMSO)¥6,732.00现货
1

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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.
[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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
130466-38-5
同义词
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
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 g/mol
溶解性
Water : ≥ 133 mg/mL (292.33 mM)
保存条件
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°C,然后在超声波浴中震荡一段时间。
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。

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