Picotamide |
Catalog No.GC18323
One-Click Copy Product Info
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Picotamide는 IC₅₀ 값이 0.76μM인 혈소판 응집 억제제이다.
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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Picotamide는 IC₅₀ 값이 0.76μM인 혈소판 응집 억제제이다. Picotamide는 트롬복산 A₂(TxA₂) 수용체와 TxA₂ 합성효소를 억제하고 혈소판 응집을 방지해서 죽상경화성 반경화의 염증 과정을 조절할 수 있다[2]. Picotamide는 혈소판 응집을 억제하는 일련의 유도체를 개발하기 위한 모델 화합물로 일반적으로 사용되고 있다[3].
체외 실험에서300μM Picotamide로 45분 처리하면 아드레날린과 트롬복산에 의해 유도된 증식성 인간 전립선 평활근 수축을 억제하였다[4]. 300μM Picotamide로 45분 처리하면 하부 비뇨기 조직에서 페닐에프린, U46619 및 전기장 자극(EFS)에 의해 유도된 평활근 수축을 억제하였다[5]. 300μM Picotamide로 30분 처리하면 돼지 신장엽간엽에서 페닐에프린에 의해 유도된 엽간 동맥의 평활근 수축을 억제하였다[6].
체내 실험에서 혈전 형성 도전 1시간 전에 단일 복강 내 투여 375mg/kg Picotamide 처리는 콜라겐과 에피네프린 정맥 주사로 인한 사망으로부터 쥐를 보호하고 순환 혈소판 수 감소와 폐 혈전 색전증을 감소시켰다[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.
| 동물 실험 [1]: | |
동물 모형 | 수컷 스위스 CD1 쥐 |
제조 방법 | 수컷 스위스 CD1 쥐(체중 20-25g)를 사육해서 사용 전 최소 1주일 동안 일반 사료를 급여하였습니다. Picotamide 또는 대조 용매는 복강(i.p.) 경로로 375mg/kg의 용량으로 투여되었습니다. Picotamide 복강 전처리 1시간 후0.154M NaCl에 용해된 콜라겐(250μg/ml)과 에피네프린(15μg/ml) 혼합물 100μl을 꼬리 정맥으로 2분 이내에 신속히 주사하였습니다. 에테르 마취 하에 심장 천자로 3.8% 구연산 삼나트륨으로 항응고된 쥐 혈액을 채취하고 원심분리해서 분석하였습니다. |
제형 | 375mg/kg 한 번; i.p. |
응용 분야 | Picotamide 처리는 폐색증이 있는 쥐의 혈액에서 순환 혈소판 수의 감소를 현저하게 감소시켰습니다. |
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 |
| Solubility | 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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
- View current batch:
- 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.)