Guanoclor
(Synonyms: 胍氯酚,Vatensol) 目录号 : GC45678
A guanidinium antihypertensive
Cas No.:5001-32-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Guanoclor is an antihypertensive agent that binds to non-adrenergic sites in pig kidney membranes (IC50 = 10 nM).1,2 It inhibits the Na+/H+ exchanger in pig kidney membranes (IC50 = 1 μM) and cell-free bovine dopamine β-hydroxylase (IC50 = 90 μM). Guanoclor inhibits electrically stimulated norepinephrine release from spleen.1 It decreases norepinephrine levels in dog heart, spleen, hypothalamus, and adrenal gland when administered at a dose of 10 mg/kg per day for six weeks. It decreases adrenal catecholamine levels in rats when administered at a dose of 20 mg/kg per day for six weeks. Guanoclor (20 mg/kg) decreases experimentally induced hypertension and the tyramine-induced pressor response and increases the norepinephrine-induced pressor response in non-anesthetized dogs.
|1. Lawrie, T.D., Lorimer, A.R., McAlpine, S.G., et al. Clinical trial and pharmacological study of compound 1029. ("Vatensol"). Br. Med. J. 1(5380), 402-406 (1964).|2. Vigne, P., Lazdunski, M., and Frelin, C. Guanabenz, guanochlor, guanoxan and idazoxan bind with high affinity to non-adrenergic sites in pig kidney membranes. Eur. J. Pharmacol. 160(2), 295-298 (1989).
| Cas No. | 5001-32-1 | SDF | |
| 别名 | 胍氯酚,Vatensol | ||
| Canonical SMILES | ClC1=C(OCCNNC(N)=N)C(Cl)=CC=C1 | ||
| 分子式 | C9H12Cl2N4O | 分子量 | 263.1 |
| 溶解度 | Soluble in DMSO | 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 | 3.8008 mL | 19.0042 mL | 38.0084 mL |
| 5 mM | 0.7602 mL | 3.8008 mL | 7.6017 mL |
| 10 mM | 0.3801 mL | 1.9004 mL | 3.8008 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。
Spectrophotometric analysis of some guanidino drugs by acid-dye and charge-transfer complexation methods
J Pharm Biomed Anal 1993 Aug;11(8):639-45.PMID:8257728DOI:10.1016/0731-7085(93)80169-2.
Two spectrophotometric methods are described for the determination of guanethidine sulphate (I), guanfacine hydrochloride (II), Guanoclor sulphate (III), guanoxan sulphate (IV) and debrisoquine sulphate (V). The first method involves ion-pair formation of the selected compounds (I-V) with bromocresol purple at pH 3.8. The yellow ion pair is extracted with chloroform and the absorbance is measured at about 415 nm. The second method is based on the reaction of the basic guanidino compounds (I, III-V) with iodine in chloroform to give molecular charge-transfer complexes with maximum absorbance at 292 and 345 nm. Beer's law was obeyed for both methods and the relative standard deviations were found to be less than 2%. The apparent molar absorptivities were found to be 2.1 x 10(4) to 6.9 x 10(4) l mol-1 cm-1 using bromocresol purple and 0.7 x 10(4) to 2.4 x 10(4) l mol-1 cm-1 using iodine. The investigated drugs were assayed in tablets. The mean percentage recoveries were found to be 99.8-100.8% by the acid-dye method and around 100.4% by the charge-transfer complexation method.
Conformational populations for antihistamines and antihypertensives in solution
J Pharm Sci 1976 Apr;65(4):612-4.PMID:5591DOI:10.1002/jps.2600650437.
The conformations in aqueous solution were determined for the XCH2CH2N systems of some antihistamines (H1-receptor antagonists) and some adrenergic neuron blocking agents, including the antihypertensive drugs guanethidine and Guanoclor. The rotameric species thought to be the pharmacologically active one is often not the only rotamer present in solution.