Propylthiouracil(6-Propyl-2-th

Propylthiouracil(6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor. Target: Thyroperoxidase (TPO) Propylthiouracil (PTU) is a thiouracil-derived drug used to treat hyperthyroidism (including Graves' disease) by decreasing the amount of thyroid hormone produced by the thyroid gland [1]. The antithyroid drug 6-propylthiouracil (PTU) was shown to have an unexpectedly prolonged inhibitory effect on iodination in the thyroid glands of rats. Eighteen hours after injection of a relatively small dose, iodination in the thyroid remained inhibited by more than 90% [2]. PTU inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin. This is one of the essential steps in the formation of thyroxine (T4). PTU does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors, such as perchlorate and thiocyanate. From Wikipedia.

170.23

C₇H₁₀N₂OS

51-52-5

丙硫氧嘧啶；丙基硫氧嘧啶；丙基硫尿嘧啶

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (587.44 mM)

H₂O : 0.67 mg/mL (3.94 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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, 6 months; -20°C, 1 month。-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。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution

• 2.

  请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution

• 3.

  请依序添加每种溶剂： 10% DMSO 90% corn oil

  Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution

• [1]. Nakamura, H., et al., Comparison of methimazole and propylthiouracil in patients with hyperthyroidism caused by Graves' disease. J Clin Endocrinol Metab, 2007. 92(6): p. 2157-62.

  [2]. Taurog, A. and M.L. Dorris, A reexamination of the proposed inactivation of thyroid peroxidase in the rat thyroid by propylthiouracil. Endocrinology, 1989. 124(6): p. 3038-42.