Benzthiazide
(Synonyms: 苄噻嗪) 目录号 : GC32634
Benzthiazide是一种长效的利尿剂和抗高血压剂。Benzthiazide为碳酸酐酶9(carbonicanhydrase9(CA9))的抑制剂，对CA9，CA2和CA1的Ki值分别为8.0，8.8和10nM。Benzthiazide能够抑制肿瘤细胞增殖。
Cas No.:91-33-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Benzthiazide is a long-acting diuretic[1] and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells[2].
Benzthiazide (0.4, 2, 10 μM) suppresses proliferation of cancer cell under hypoxic conditions in a dose-dependent manner. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively[2].
Benzthiazide (1, 1.5 mg/100 g BW) causes a marked decrease in urinary calcium excretion and the dissociation of calcium and sodium excretion in hyperprolactinemic rats[1].
[1]. Adler RA, et al. Hypercalciuria in hyperprolactinemic rats: effects of benzthiazide. Metabolism. 1986 Jul;35(7):668-72. [2]. Lee HS, et al. Rational drug repositioning guided by an integrated pharmacological network of protein, disease and drug. BMC Syst Biol. 2012 Jul 2;6:80.
| Cas No. | 91-33-8 | SDF | |
| 别名 | 苄噻嗪 | ||
| Canonical SMILES | O=S(C1=C(Cl)C=C(C2=C1)NC(CSCC3=CC=CC=C3)=NS2(=O)=O)(N)=O | ||
| 分子式 | C15H14ClN3O4S3 | 分子量 | 431.94 |
| 溶解度 | DMSO: 50 mg/mL (115.76 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 | 2.3151 mL | 11.5757 mL | 23.1514 mL |
| 5 mM | 0.463 mL | 2.3151 mL | 4.6303 mL |
| 10 mM | 0.2315 mL | 1.1576 mL | 2.3151 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。
Hypercalciuria in hyperprolactinemic rats: effects of Benzthiazide
Metabolism 1986 Jul;35(7):668-72.PMID:3724459DOI:10.1016/0026-0495(86)90176-9.
There is evidence that prolactin (PRL) excess plays a role in the etiology of osteoporosis associated with human prolactinoma. Calcium balance in human hyperprolactinemia has not been thoroughly investigated. In the present study, rats with excess circulating PRL levels (male anterior pituitary-grafted Fischer 344 rats) had urinary calcium excretion twice that of control rats (4.16 +/- 0.43 v 2.25 +/- 0.30 mg/24h X 100 g BW). Calcium excretion expressed per mg of calcium intake was also high in pituitary-grafted rats. The excess calcium excretion in hyperprolactinemic rats was not accompanied by a concomitant rise in sodium excretion. This dissociation suggests that PRL has an effect on the renal handling of calcium. Since thiazide diuretics have a well-described hypocalciuric action, their effect was tested in these rats. In normal rats, Benzthiazide, a long-acting agent, significantly reduced urinary calcium excretion in a dose-dependent fashion. Hyperprolactinemic rats responded to Benzthiazide in a manner similar to control rats. In pituitary-grafted rats, Benzthiazide also decreased the calcium excretion to intake ratio and normalized the calcium to sodium excretion ratio. Since the hypercalciuria of experimental hyperprolactinemia can be corrected by thiazide diuretics, these agents may have therapeutic potential in human PRL excess.
HPLC determination of Benzthiazide in biologic material
Biopharm Drug Dispos 1982 Jan-Mar;3(1):1-9.PMID:7082774DOI:10.1002/bdd.2510030102.
An assay was developed for Benzthiazide in plasma, urine and feces, using high performance liquid chromatography (HPLC). A reverse-phase column was employed, with quantitation af 280 nm, using polythiazide as an internal standard. In three of four human subjects who received a 50 mg Benzthiazide tablet the plasma concentrations were below the 10 ng ml-1 sensitivity limit of the assay, and the urinary recovery averaged less than one per cent of the dose. One subject received a 50 mg dose as both a tablet and a solution; the urinary recoveries for these two doses were 1.7 and 10.4 per cent, respectively. Fecal samples, obtained from two subjects who received 50 mg tablets, were estimated to contain approximately 80 per cent of the administered dose.