Picotamide |
カタログ番号GC18323
One-Click Copy Product Info
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Picotamideは血小板凝集阻害剤であり、IC50値は0.76μMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 32828-81-2
Sample solution is provided at 25 µL, 10mM.
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Picotamideは血小板凝集阻害剤であり、IC50値は0.76μMである[1]。Picotamideは、トロンボキサンA2（TxA2）受容体とTxA2合成酵素を阻害し、血小板の凝集を予防し、動脈硬化性プラークの炎症プロセスを調節する[2]。Picotamideは、モデル化合物として広く使われ、血小板の凝集を阻害するための一連の誘導体を開発する[3]。
In vitro（体外）実験で、300μMのPicotamideで45分間処理したところ、アドレナリン作動薬とトロンボキサンに誘発されたヒト前立腺肥大平滑筋の収縮を阻害した[4]。300μM Picotamideで45分間処理したところ、下部尿路組織で、フェニレフリン、U46619と電場刺激（EFS）による平滑筋の収縮が阻害された[5]。300μM Picotamideで30分間処理したところ、phenylephrineによる豚の腎臓の葉間部で、小葉間動脈の平滑筋の収縮が阻害された[6]。
In vivo（体内）実験で、血栓症のチャレンジの1時間前に、単回用量が375mg/kgのPicotamideを腹腔内注射すれば、コラーゲン+エピネフリンの静脈内注射による死亡からマウスを保護でき、循環血小板数の減少と肺血栓塞栓症が軽減された[7]。
References:
[1] Liu X J, Shi X X, Zhong Y L, et al. Design, synthesis and in vitro activities on anti-platelet aggregation of 4-methoxybenzene-1, 3-isophthalamides[J]. Bioorganic & medicinal chemistry letters, 2012, 22(21): 6591-6595.
[2] Celestini A, Violi F. A review of picotamide in the reduction of cardiovascular events in diabetic patients[J]. Vascular Health and Risk Management, 2007, 3(1): 93-98.
[3] Zou J, Gao P, Hao X, et al. Recent progress in the structural modification and pharmacological activities of ligustrazine derivatives[J]. European Journal of Medicinal Chemistry, 2018, 147: 150-162.
[4] Hennenberg M, Miljak M, Herrmann D, et al. The receptor antagonist picotamide inhibits adrenergic and thromboxane-induced contraction of hyperplastic human prostate smooth muscle[J]. American Journal of Physiology-Renal Physiology, 2013, 305(10): F1383-F1390.
[5] Hennenberg M, Tamalunas A, Wang Y, et al. Inhibition of agonist-induced smooth muscle contraction by picotamide in the male human lower urinary tract outflow region[J]. European journal of pharmacology, 2017, 803: 39-47.
[6] Li B, Huang R, Wang R, et al. Picotamide inhibits a wide spectrum of agonist‐induced smooth muscle contractions in porcine renal interlobar and coronary arteries[J]. Pharmacology Research & Perspectives, 2021, 9(3): e00771.
[7] Gresele P, Corona C, Alberti P, et al. Picotamide protects mice from death in a pulmonary embolism model by a mechanism independent from thromboxane suppression[J]. Thrombosis and haemostasis, 1990, 64(05): 080-086.
| 動物実験 [1]: | |
動物モデル | 雄のSwiss CD1マウス |
準備方法 | 使用の前に、体重が20-25gの雄のSwiss CD1マウスをケージに入れ、通常の飼料を少なくとも1週間飼育した。用量が375mg/kgのPicotamideまたは溶媒を腹腔内（i. p.）投与した。Picotamideの腹腔内前処理の1時間後、0.154M NaClの中の100μlのコラーゲン（250μg/ml）とエピネフリン（15μg/ml）の混合液を、尾静脈に速やかに（2分間以内）注射した。3.8%のクエン酸三ナトリウムで抗凝固処理したマウス血液を、エーテル麻酔の下で、心臓穿刺で採取し、分析のために遠心分離した。 |
投与形態 | 375mg/kg、単回；腹腔内注射 |
アプリケーション | Picotamideの処理により、肺塞栓症のマウスの血液で、循環血小板の数の減少が著しく減った。 |
References: | |
| Cas No. | 32828-81-2 | SDF | |
| Chemical Name | 4-methoxy-N1,N3-bis(3-pyridinylmethyl)-1,3-benzenedicarboxamide | ||
| Canonical SMILES | O=C(C1=CC=C(OC)C(C(NCC2=CC=CN=C2)=O)=C1)NCC3=CN=CC=C3 | ||
| Formula | C21H20N4O3 | M.Wt | 376.4 |
| 溶解度 | 1mg/mL in ethanol, 5mg/ml in DMSO, 10mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6567 mL | 13.2837 mL | 26.5675 mL |
| 5 mM | 531.3 μL | 2.6567 mL | 5.3135 mL |
| 10 mM | 265.7 μL | 1.3284 mL | 2.6567 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)