Desfesoterodine
(Synonyms: (R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine) 目录号 : GC358425-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM,Desfesoterodine) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
Cas No.:207679-81-0
Sample solution is provided at 25 µL, 10mM.
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM,Desfesoterodine) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. [1] 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3]
5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. [1]
[1] Nilvebrant L, et al. Pharmacol Toxicol, 1997, 81(4), 169-172. [2] Nilvebrant L, et al. Life Sci, 1997, 60(13-14), 1129-1136. [3] Modiri AR, et al. Urology, 2002, 59(6), 963-968.
Cas No. | 207679-81-0 | SDF | |
别名 | (R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine | ||
Canonical SMILES | OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C | ||
分子式 | C22H31NO2 | 分子量 | 341.49 |
溶解度 | DMSO: ≥ 100 mg/mL (292.83 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9283 mL | 14.6417 mL | 29.2834 mL |
5 mM | 0.5857 mL | 2.9283 mL | 5.8567 mL |
10 mM | 0.2928 mL | 1.4642 mL | 2.9283 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 | |||
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% 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。
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Quality Control & SDS
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- Purity: >99.00%
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