GLPBio

Phenamil

Catalog No.: GC13994Purity:>98.00%
COASDSData Sheet
الفيناميل ، وهو نظير لأميلوريد ، هو مانع لقنوات الصوديوم الظهارية (ENaC) أكثر فعالية وأقل قابلية للعكس مع IC50 من 400 نانومتر.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

Phenamil
Cas No.: 1161-94-0
5mgIn Stock
$83.00
1
10mgIn Stock
$117.00
1
50mgIn Stock
$490.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

المراجع (Citations)

1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتج

الوصف (Description)

Phenamil is a selective inhibitor of transient receptor potentials (TRPs) and acid-sensing ion channels (ASICs) [1]. Phenamil is an amiloride analogs and a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM [2]. Phenamil inhibited TRPP3 -mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay [3].

Phenamil (10 µM) Treatment of M2-10B4 (M2) mouse (mesenchymal stem cells) MSCs for 6 days with 10 µM phenamil markedly stimulated expression of the genes encoding ALP, Runx2, OCN, and osterix. Phenamil induces osteogenic gene expression and mineralization in both MSC and primary calvariae organ cultures [4]. Phenamil (10 µM) induced the expression of PPARγ within 24 h in 3T3-F442A preadipocyte cell lines. Phenamil act as a new proadipogenic compound [5].

Phenamil (15 or 30 mg/kg; 21 days) reduced chronic-hypoxia-induced pulmonary artery hypertension (PAH). Infusion of phenamil during hypoxia treatment inhibited pulmonary vascular remodeling [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.

البروتوكول (Protocol)

Cell experiment [1]:

Cell lines

Osteoblast-like MC3T3-E1 cells

Preparation Method

The cells were maintained in regular growth medium, i.e. α-minimal essential medium supplemented with 10% fetal bovine serum (FBS), 100 U/ml penicillin G and 100 mg/ml streptomycin. The culture medium, with or without 10 µM phenamil, was replaced every 3-4 days.

Reaction Conditions

10 µM for 14 days

Applications

Phenamil-treated and -untreated control cells showed a statistically significant increase in cell proliferation from day 7 to day 14.
Animal experiment [2]:

Animal models

Male Sprague-Dawley rats

Preparation Method

Miniature osmotic infusion pumps which deliver saline-DMSO (50% saline-50% DMSO) solution or phenamil in saline-DMSO were implanted subcutaneously in male Sprague-Dawley rats (age, 6 to 7 weeks; weight, 250 to 300 g) between the scapulae and connected via a catheter advanced into the left carotid artery. Four rats were used for each condition. Phenamil (15 or 30 mg/kg of body weight/day) was administered continuously for 21 days at an infusion rate of 1 ml/h. The rats were subjected to hypobaric hypoxia (10.5% oxygen) or normoxia (room air) for 21 days.

Dosage form

15 or 30 mg/kg, Miniature osmotic infusion pump

Applications

Phenamil reduces chronic-hypoxia-induced pulmonary artery hypertension (PAH).

References:

[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.

وثائق المنتج (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1161-94-0
الاسم الكيميائي
(E)-3,5-diamino-N-(amino(phenylamino)methylene)-6-chloropyrazine-2-carboxamide methanesulfonate
SMILES
ClC(N=C1C(/N=C(N)/NC2=CC=CC=C2)=O)=C(N)N=C1N.OS(=O)(C)=O
الصيغة الجزيئية
C12H12ClN7O.CH3SO3H
الوزن الجزيئي
401.83
الذوبانية
DMF: 0.1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

Reviews

Review for Phenamil

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%