Hyoscyamine

製品コードS4014 バッチS401401

印刷

化学情報

Chemical Structure Synonyms Daturine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H23NO3
分子量 289.37 CAS No. 101-31-5
Solubility (25°C)* 体外 DMSO 58 mg/mL (200.43 mM)
Ethanol 58 mg/mL (200.43 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
30%propylene glycol 5%Tween80 65%D5W

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (17.28mM) Taking the 1 mL working solution as an example, add 300 μL of clarified propylene glycol stock solution of 16.67 mg/ml to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.
in vitro L-hyoscyamine increases the turnover number of GTPase activity from 0.19 min-1 to 2.11 min-1 in the steady-state kinetic measurements. [2] R-(+)-hyoscyamine results in displacement of [3H]NMS binding to the muscarinic acetylcholine receptor subtypes (m1-m5) with pKi value of 8.67, 8.51, 7.46, 8.56 and 8.53, respectively. [3] Hyoscyamine prevents the agonist-induced stimulation of cAMP production with EC50 of 7.8 nM in CHO cells. [4] S-(-)-hyoscyamine enhances the forskolin-stimulated synthesis of cyclic AMP in rat cardiac (both atrial and ventricular) membranes by up to 24%. [5]
in vivo L-hyoscyamine (20 mg/kg) prolongs migrating myoelectric complex (MMC) cycle length from 17.6 min to 29.0 min in conscious rats. [6]
特徴 R-(+)-hyoscyamine is 30-fold lower in potency than that of the S-(-) enantiomer.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
Membrane preparation containing 500 μg protein in a final volume of 500 μL is incubated with 3H quinuclidinyl benzilate (QNB) (44 Ci/mmol) for 60 min at 20 ℃ in the absence and presence of 2 μmol atropine as blank. the incubation is stopped with 3 mL icecold 0.9% NaCl solution and filtered through Whatman GF/C glass fiber filters with suction. The filters are washed three times with 3 mL icecold 0.9% NaCl solution, placed in vials, dried for 30 min at 60 ℃ and extracted with Ultima Gold scintillation cocktail for 1 hour. Radioactivity is measured in scintillation counter.
動物実験 動物モデル Rats
投薬量 20 mg/kg
投与方法 Intravenous injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/7675895/
  • https://pubmed.ncbi.nlm.nih.gov/3126798/
  • https://pubmed.ncbi.nlm.nih.gov/7616422/
  • https://pubmed.ncbi.nlm.nih.gov/7797541/
  • https://pubmed.ncbi.nlm.nih.gov/12108922/
  • https://pubmed.ncbi.nlm.nih.gov/12706477/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Co-delivery of phagocytosis checkpoint and STING agonist by a Trojan horse nanocapsule for orthotopic glioma immunotherapy [ Theranostics, 2022, 12(12):5488-5503] PubMed: 35910792

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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