Phenamil |
| Catalog No.GC13994 |
Phenamil는 TRPs (transient receptor potentials)및 ASICs (acid-sensing ion channel)을 선택적으로 억제하는 억제제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1161-94-0
Sample solution is provided at 25 µL, 10mM.
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Phenamil는 TRPs (transient receptor potentials)및 ASICs (acid-sensing ion channel)을 선택적으로 억제하는 억제제이다.Phenamil는 아밀로리 유사물질이며 IC50이 400 nM인 강력하고 되돌릴 수 없는 상피 나트륨 통도(ENaC) 차단제이다 [2]. Phenamil는 Ca2+ uptake assay에서 IC50 140 nM으로 TRPP3에 의한 Ca2+ 운송을 억제했다 [3].
Phenamil (10 µM)는 M2-10B4(M2) 쥐(간질세포) 유동 세포(MSCs)에 6일 동안 10 µM Phenamil 처리를 통해 ALP, Runx2, OCN, 그리고 osterix을 인코딩하는 유전자의 표현을 현저하게 자극했다. Phenamil는 MSC와 calvariae 기관 문화에서 성골 유전자 표현과 미네랄화를 유도한다 [4]. Phenamil (10 µM)는 3T3-F442A preadipocyte세포에서 24시간 내에 PPARγ의 표현을 유도한다. Phenamil는 새로운 지방 생성 프로콥팜드로 작용한다 [5].
Phenamil (15 또는 30 mg/kg; 21일)는 만성 저산소 유발의 고혈압 (PAH)을 감소시켰다. Phenamil를 저산소 치료 중 투여함으로써 폐혈관 재구성 과정을 억제했다[6].
References:
[1]. Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530.
[2]. Hirsh A J, Molino B F, Zhang J, et al. Design, synthesis, and structure− activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis[J]. Journal of medicinal chemistry, 2006, 49(14): 4098-4115.
[3]. Dai X Q, Ramji A, Liu Y, et al. Inhibition of TRPP3 channel by amiloride and analogs[J]. Molecular pharmacology, 2007, 72(6): 1576-1585.
[4]. Park K W, Waki H, Kim W K, et al. The small molecule phenamil induces osteoblast differentiation and mineralization[J]. Molecular and cellular biology, 2009, 29(14): 3905-3914.
[5]. Park K W, Waki H, Choi S P, et al. The small molecule phenamil is a modulator of adipocyte differentiation and PPARγ expression [S][J]. Journal of lipid research, 2010, 51(9): 2775-2784.
[6]. Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530.
| 세포 실험 [1]: | |
세포 라인 | 유사 골 생성 세포 MC3T3-E1 세포 |
제조 방법 | 세포는 10% 태태 소혈청(FBS), 100 U/ml 페니실린 G 및 100 mg/ml 스트레프토마이신을 보충한 α-최소 필수 매체에서 유지되었습니다. 10 µM phenamil을 포함한 여부에 관계없이 배양매체는 3~4일마다 교체되었습니다. |
반응 조건 | 10 µM ,14일 동안 |
응용 분야 | Phenamil 처리 및 미처리 대조 세포는 7일부터 14일까지 세포 증식이 통계적으로 유의한 증가를 보였습니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 Sprague-Dawley 쥐 |
제조 방법 | Miniature osmotic infusion 펌프는 생리식염수-DMSO(50% 생리식염수-50% DMSO) 용액 또는 생리식염수-DMSO에 의해 Phenamil을 탑재한 후, 쥐가 6~7주, 몸무게 250~300 g의 암컷 Sprague-Dawley 쥐의 등뼈 사이에 하부 피질 주사로 삽입되었으며, 왼쪽 경동맥으로 진입하는 캐시터를 통해 연결되어 있습니다. 각 조건에 대해 쥐 4마리가 사용되었습니다. Phenamil (체중별 15 또는 30mg/kg/일)은 21일 동안 1 ml/h의 흐름 속도로 지속적으로 투여되었습니다. 이들 쥐는 낮은 산소 환경(10.5% 산소) 또는 정상 산소 환경(실내 공기)에서 21일 동안 유지되었습니다. |
제형 | 15 or 30 mg/kg, Miniature osmotic infusion pump |
응용 분야 | Phenamil은 만성 희석증에 의해 유발된 폐동맥고압(PAH)을 감소시킵니다. |
참고문헌: [1] : Lo K W H, Ulery B D, Kan H M, et al. Evaluating the feasibility of utilizing the small molecule phenamil as a novel biofactor for bone regenerative engineering[J]. Journal of tissue engineering and regenerative medicine, 2014, 8(9): 728-736. [2] :Chan M C, Weisman A S, Kang H, et al. The amiloride derivative phenamil attenuates pulmonary vascular remodeling by activating NFAT and the bone morphogenetic protein signaling pathway[J]. Molecular and cellular biology, 2011, 31(3): 517-530. | |
| Cas No. | 1161-94-0 | SDF | |
| Chemical Name | (E)-3,5-diamino-N-(amino(phenylamino)methylene)-6-chloropyrazine-2-carboxamide methanesulfonate | ||
| Canonical SMILES | ClC(N=C1C(/N=C(N)/NC2=CC=CC=C2)=O)=C(N)N=C1N.OS(=O)(C)=O | ||
| Formula | C12H12ClN7O.CH3SO3H | M.Wt | 401.83 |
| Solubility | DMF: 0.1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4886 mL | 12.4431 mL | 24.8861 mL |
| 5 mM | 497.7 μL | 2.4886 mL | 4.9772 mL |
| 10 mM | 248.9 μL | 1.2443 mL | 2.4886 mL |
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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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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