Benzylthiouracil
(Synonyms: 6-Benzyl-2-thiouracil) 目录号 : GC66193
Benzylthiouracil 是一种抗甲状腺功能亢进的活性药物成分。
Cas No.:6336-50-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Benzylthiouracil is an active pharmaceutical ingredient against hyperthyroidism[1].
| Cas No. | 6336-50-1 | SDF | Download SDF |
| 别名 | 6-Benzyl-2-thiouracil | ||
| 分子式 | C11H10N2OS | 分子量 | 218.27 |
| 溶解度 | DMSO : 200 mg/mL (916.30 mM; Need ultrasonic and warming) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.5815 mL | 22.9074 mL | 45.8148 mL |
| 5 mM | 0.9163 mL | 4.5815 mL | 9.163 mL |
| 10 mM | 0.4581 mL | 2.2907 mL | 4.5815 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。
[Benzylthiouracil-induced antineutrophil cytoplasmic antibody-associated cutaneous vasculitis: a case report and literature review]
Rev Med Interne 2013 Sep;34(9):561-4.PMID:23827012DOI:10.1016/j.revmed.2013.05.012.
Introduction: Vasculitis associated to antineutrophil cytoplasmic antibodies is a rare complication of therapy with antithyroid medication. They were mainly reported in patients treated with propylthiouracil and rarely with Benzylthiouracil. Case report: We report a 22-year-old woman treated with Benzylthiouracil for Graves' disease, who developed a vasculitic skin involvement. The presence of antineutrophil cytoplasmic antibodies with anti-myeloperoxidase specificity was documented. The discontinuation of Benzylthiouracil was followed by a complete disappearance of skin lesions and of antineutrophil cytoplasmic antibodies. Conclusion: To our knowledge, only ten cases of antineutrophil cytoplasmic antibodies vasculitis induced by Benzylthiouracil have been previously reported in the literature. Our patient was characterized by the occurrence of isolated cutaneous vasculitis, without renal involvement. Early discontinuation of Benzylthiouracil may have prevented the occurrence of severe visceral complication.
Polymorphism of Benzylthiouracil, an active pharmaceutical ingredient against hyperthyroidism
Int J Pharm 2021 Apr 1;598:120378.PMID:33581273DOI:10.1016/j.ijpharm.2021.120378.
The crystal structures of dimorphic Benzylthiouracil, a drug against hyperthyroidism, have been redetermined and the atom coordinates of the two independent molecules of form I have been obtained for the first time. The dimorphism convincingly demonstrates the conformational versatility of the Benzylthiouracil molecule. It has been established through calorimetric studies that the low-temperature form II transforms endothermically (ΔII→IH = 5.6(1.5) J g-1) into form I at 405.4(1.0) K. The high-temperature form I melts at 496.8(1.0) K (ΔI→LH = 152.6(4.0) J g-1). Crystallographic and thermal expansion studies show that form II is denser than form I, leading to the conclusion that the slope of the II-I equilibrium curve in the pressure-temperature phase diagram is positive. It follows that this dimorphism corresponds to a case of overall enantiotropic behaviour, which implies that both solid phases possess their own stable phase region irrespective of the pressure. Moreover, form II is clearly the stable polymorph under ambient conditions.
Benzylthiouracil-induced ANCA-associated Vasculitis: A Case Report and Literature Review
Eur J Case Rep Intern Med 2019 Dec 10;6(12):001283.PMID:31893199DOI:10.12890/2019_001283.
Iatrogenic antineutrophil cytoplasm antibody (ANCA)-associated vasculitis (AAV) is not exceptional. Many cases of small vessel vasculitis induced by anti-thyroid drugs (ATD), mainly propylthiouracil (PTU), have been reported. We present a case of AAV related to another ATD: Benzylthiouracil (BTU) and review the literature. An 84-year-old man with a 4-year history of multinodular goitre with hyperthyroidism was treated with BTU. He presented an acute syndrome with weakness, fever, epigastric pain and abdominal distension. Lactate and lipase tests were normal. An abdominal scan showed a thrombosis of the splenic artery with splenic infarction. We excluded a hypothesis of associated embolic aetiology: atrial fibrillation, atrial myxoma, intraventricular thrombus or artery aneurysm. Exploration of a possible prothrombotic state (complete blood count, haemostasis tests, activated protein C resistance, factor V Leiden, protein C, S, antithrombin III) gave normal results. Tests for antinuclear antibodies (ANA) and antiphospholipid antibodies (APL) were negative. However, testing for p-ANCA, with antimyeloperoxidase (MPO) specificity, was positive: 120.6 CU (N<20.0). We did not find other systemic manifestations, except a non-specific kidney failure. BTU was discontinued without steroids or immune-modulating drugs. Subsequently, symptoms disappeared progressively and titres of ANCA fell until normalization, 4 months later. Many patients treated with BTU present a high prevalence of ANCA, mainly, but not exclusively, directed against MPO. Vasculitis, however, remains an uncommon complication. The mechanism of this anomaly remains to be elucidated. Some studies suggest the possibility of an autoimmune reaction initiated by drug bioactivation mediated by neutrophil-derived MPO. The present observation is particular because the involved drug was BTU and clinical expression was unusual. Learning points: ANCA-associated vasculitis related to anti-thyroid drugs is not exceptional, particularly in patients receiving long-term therapy with thioamides.Clinical manifestations are highly variable.Treatment consists firstly of stopping the anti-thyroid drug. Introduction of steroids and/or immunosuppressive therapy depends on the severity of organic impairments. Prognosis is less severe than primary ANCA vasculitis.
Benzylthiouracil induced ANCA associated glomerulonephritis in patients with graves' disease
Tunis Med 2015 Nov;93(11):696-701.PMID:27126427doi
Background: Renal complications in Graves' disease are rare and may be related either to the disease itself or secondary to antithyroid drugs. Aim: We report 6 cases of renal damage in patients with Graves' disease treated with Benzylthiouracil collected over a period of 14 years. Methods: There were 6 women with a mean age of 37.86 ± 14.25 years. All patients developed renal vasculitis associated with ANCA. The signs were dominated by renal proteinuria and renal failure associated with hematuria in all cases. The lung involvement was the most common extrarenal manifestation occurred in 4 patients (alveolar hemorrhage in 2 cases, lymphocytic alveolitis in 1 case and pleurisy in 1 case). The Benzylthiouracil was discontinued in 3 patients still under treatment. Corticosteroid therapy was used alone or in combination with cyclophosphamide in all cases. Plasmapheresis sessions were made during the alveolar hemorrhage. A complete remission was obtained in one case and incomplete remission in 2 cases. The other 3 patients required chronic hemodialysis. One patient died of sepsis. Conclusion: The possibility of renal impairment in antithyroid drugs treated Graves' disease requires monitoring to detect urinary abnormalities in order to early initiate therapy and improve patient's outcome.
[Vasculitis with renal and pulmonary involvement in a patient receiving Benzylthiouracil for Graves disease]
Rev Med Interne 2002 Oct;23(10):857-61.PMID:12428490DOI:10.1016/s0248-8663(02)00704-x.
Introduction: Vasculitis is a rare complication of antithyroid drugs reported with propylthiouracil, carbimazole, methimazole and we describe the first case with benzylthyouracil. Renal involvement during thyroid auto-immune diseases and during vasculitis as complication of antithyroid drugs will be discussed. Exegesis: We present a case study of 28-year-old female patient with Graves' disease diagnosed in 1996 and treated by Benzylthiouracil for 2 years. The thyroid function was poorly controlled, so surgical treatment was indicated in May 1998. One month later, she developed vasculitis with pulmonary and renal involvement. Her renal function deteriorated rapidly. On admission, the additional laboratory findings showed hematuria, proteinuria of 1.44 g/day and serum creatinine level at 1000 mumol/l. She had myeloperoxidase-anti neutrophil cytoplasmic antibody, antithyroglobulin and antimicrosome antibodies. A renal biopsy revealed pauci-immune crescentic glomerulonephritis with 75% sclerous crescents. Chest-X-ray showed unilateral alveolar shadowing and a bronchio-alveolar lavage revealed lymphocytic alveolitis. She was treated with high dose of prednisolone and cyclophosphamide. After a follow-up of 18 months, the serum creatinine level decreased at 186 mumol/l and chest-X-ray returned to normal. Conclusion: Some cases of vasculitis associated with anti-thyroid drug treatment are reported.