B-HT 933 dihydrochloride
(Synonyms: B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) 目录号 : GC14514
An α2-AR agonist
Cas No.:36067-72-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.44 μM
The contractile effects of adrenaline and noradrenaline may be mediated by both postjunctional α2- and α2-adrenoceptors on vascular smooth muscle. B-HT 933 is a selective α2-adrenoceptor agonist.
In vitro: B-HT 933, a selective α2-adrenoceptor agonist, contracts human subcutaneous resistance arteries by a mechanism largely dependent on the influx of extracellular Ca2+, probably through voltage-operated calcium channels. This action involves a pertussis toxin-sensitive G protein, possibly GQ [1].
In vivo: The dose-related effects of the selective α2-adrenoceptor agonist B-HT 933 on the body temperature of untreated and reserpine-treated mice were investigated. In untreated mice B-HT 933 induced a dose-related hypothermia. The highest dose of B-HT 933 elicited a marked hypothermia, whereas the maximal hypothermic effect of clonidine was less pronounced and reached a plateau at a dose of 0.5 mg/kg [2].
Clinical trial: Up to now, B-HT 933 is still in the preclinical development stage.
Reference:
[1] N. A. Parkinson & A.D. Hughes. The mechanism of action of 1c2-adrenoceptors in human isolated subcutaneous resistance arteries. British Journal of Pharmacology (1995) 115, 1463-1468
[2] D. J. Bill, I.E. Hughes & R.J. Stephens. The thermogenic actions of x2-adrenoceptor agonists in reserpinized mice are mediated via a central postsynaptic ac2-adrenoceptor mechanism. Br. J. Pharmacol. (1989), 96, 133-143
| Cas No. | 36067-72-8 | SDF | |
| 别名 | B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride | ||
| 化学名 | 6-ethyl-5,6,7,8-tetrahydro-4H-oxazolo[4,5-d]azepin-2-amine dihydrochloride | ||
| Canonical SMILES | NC1=NC2=C(CCN(CC)CC2)O1.Cl.Cl | ||
| 分子式 | C9H15N3O.2HCl | 分子量 | 254.16 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml | 储存条件 | Desiccate at RT |
| 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 | 3.9345 mL | 19.6726 mL | 39.3453 mL |
| 5 mM | 0.7869 mL | 3.9345 mL | 7.8691 mL |
| 10 mM | 0.3935 mL | 1.9673 mL | 3.9345 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。