RAAS

シグナル伝達経路

研究分野

阻害剤の選択性比較
溶解度

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2199	Aliskiren Hemifumarate	100 mg/mL	100 mg/mL	100 mg/mL
S1657	Enalaprilat Dihydrate	<1 mg/mL	70 mg/mL	<1 mg/mL
S5067	Losartan	-1 mg/mL	84 mg/mL	-1 mg/mL
S5728	Delapril Hydrochloride	<1 mg/mL	98 mg/mL	25 mg/mL
S5712	Zofenopril calcium	<1 mg/mL	32 mg/mL	<1 mg/mL
S1506	Perindopril Erbumine	88 mg/mL	<1 mg/mL	88 mg/mL
S1793	Ramipril	<1 mg/mL	83 mg/mL	83 mg/mL
S1941	Enalapril Maleate	<1 mg/mL	99 mg/mL	4 mg/mL
S2051	Captopril	2 mg/mL	43 mg/mL	43 mg/mL
S2076	Lisinopril	20 mg/mL	<1 mg/mL	<1 mg/mL
S2081	Cilazapril Monohydrate	<1 mg/mL	87 mg/mL	87 mg/mL
S2079	Moexipril HCl	<1 mg/mL	20 mg/mL	<1 mg/mL
S2581	Quinapril HCl	95 mg/mL	18 mg/mL	95 mg/mL
S2099	Temocapril HCl	<1 mg/mL	103 mg/mL	103 mg/mL
S2109	Imidapril HCl	54 mg/mL	88 mg/mL	29 mg/mL
S7678	LCZ696	100 mg/mL	30 mg/mL	9 mg/mL
S2095	Fosinopril Sodium	117 mg/mL	<1 mg/mL	4 mg/mL
S1578	Candesartan	<1 mg/mL	88 mg/mL	1 mg/mL
S1359	Losartan Potassium (DuP 753)	92 mg/mL	92 mg/mL	92 mg/mL
S1738	Telmisartan	<1 mg/mL	13 mg/mL	<1 mg/mL
S4975	Fimasartan	-1 mg/mL	100 mg/mL	24 mg/mL
S1507	Irbesartan	<1 mg/mL	4 mg/mL	3 mg/mL
S1894	Valsartan	<1 mg/mL	87 mg/mL	87 mg/mL
S7098	PD123319	100 mg/mL	100 mg/mL	100 mg/mL
S1604	Olmesartan Medoxomil	<1 mg/mL	89 mg/mL	<1 mg/mL
S2037	Candesartan Cilexetil	<1 mg/mL	122 mg/mL	4 mg/mL
S3057	Azilsartan Medoxomil	<1 mg/mL	114 mg/mL	<1 mg/mL
S3046	Azilsartan	<1 mg/mL	91 mg/mL	<1 mg/mL
S4102	Eprosartan Mesylate	<1 mg/mL	104 mg/mL	4 mg/mL
S2199	Aliskiren Hemifumarate	100 mg/mL	100 mg/mL	100 mg/mL
S1657	Enalaprilat Dihydrate	<1 mg/mL	70 mg/mL	<1 mg/mL
S5067	Losartan	-1 mg/mL	84 mg/mL	-1 mg/mL
S5728	Delapril Hydrochloride	<1 mg/mL	98 mg/mL	25 mg/mL
S5712	Zofenopril calcium	<1 mg/mL	32 mg/mL	<1 mg/mL
S1506	Perindopril Erbumine	88 mg/mL	<1 mg/mL	88 mg/mL
S1793	Ramipril	<1 mg/mL	83 mg/mL	83 mg/mL
S1941	Enalapril Maleate	<1 mg/mL	99 mg/mL	4 mg/mL
S2051	Captopril	2 mg/mL	43 mg/mL	43 mg/mL
S2076	Lisinopril	20 mg/mL	<1 mg/mL	<1 mg/mL
S2081	Cilazapril Monohydrate	<1 mg/mL	87 mg/mL	87 mg/mL
S2079	Moexipril HCl	<1 mg/mL	20 mg/mL	<1 mg/mL
S2581	Quinapril HCl	95 mg/mL	18 mg/mL	95 mg/mL
S2099	Temocapril HCl	<1 mg/mL	103 mg/mL	103 mg/mL
S2109	Imidapril HCl	54 mg/mL	88 mg/mL	29 mg/mL
S7678	LCZ696	100 mg/mL	30 mg/mL	9 mg/mL
S2095	Fosinopril Sodium	117 mg/mL	<1 mg/mL	4 mg/mL

亜型選択性的な製品

RAAS阻害剤(48)
新RAAS製品

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2199	Aliskiren Hemifumarate Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.
S1657	Enalaprilat Dihydrate Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.
S5067^新	Losartan Losartan is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement.
S5728^新	Delapril Hydrochloride
S5712^新	Zofenopril calcium Zofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.
S1506	Perindopril Erbumine Perindopril Erbumine is a potent ACE inhibitor with IC50 of 1.05 nM.
S1793	Ramipril Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
S1941	Enalapril Maleate Enalapril Maleate is an angiotensin-converting enzyme (ACE) inhibitor, used in the treatment of hypertension, diabetic nephropathy, and chronic heart failure.
S2051	Captopril Captopril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 6 nM.
S2076	Lisinopril Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
S2081	Cilazapril Monohydrate Cilazapril Monohydrate is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
S2079	Moexipril HCl Moexipril HCl is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure.
S2581	Quinapril HCl Quinapril HCl is the hydrochloride salt of quinapril that is an angiotensin-converting enzyme inhibitor with a Ki of 20 μM.
S2099	Temocapril HCl Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.
S2100	Temocapril Temocapril is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.
S2109	Imidapril HCl Imidapril HCl is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 2.6 nM, used for the treatment of hypertension.
S7678	LCZ696 Sacubitril/valsartan (LCZ696), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.	J Mol Cell Cardiol, 2017, 108:138-148	Histological analysis staining of three groups. (a) Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×200). (b) Masson staining of three groups (original magnification ×200). Collagen content (%) of heart tissues were presented as fibrosis (**P < 0.001, n = 7 per group). (c) Cardiac section of three group mice hearts stained with WGA (original magnification ×400) (P < 0.05, n = 7 per group). (d) The expression of Drp1 significantly increased in DOX group (*P < 0.001, n = 7 per group) and it decreased in DOX + LCZ696 group (P < 0.01, n = 7 per group).
S2095	Fosinopril Sodium Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
S1578	Candesartan Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.	Exp Biol Med, 2015, 10.1177/1535370215576312 Acta Biochim Biophys Sin, 2015, 47(7), 1–9 Sci Rep, 2015, 5:8116	In vivo effects of candesartan and valsartan in post-MI rats overexpressing adrenal barr1. (A) Trichrome-Masson's staining in myocardial cross-sections from post-MI rats overexpressing barr1 specifically in their adrenals and treated for 7 days with either vehicle or 10 mg/kg body weight/day candesartan or 40 mg/kg body weight/day irbesartan (all via drinking water). Blue denotes collagen fibers, red denotes muscle fibers, and black represents cell nuclei. Representative images are shown from 5–6 rat hearts stained per group, along with staining in sham-operated rat hearts, in which no blue staining was detectable. (B,C) Heart mRNA levels of (B) collagen I (Col1a1) and brain natriuretic peptide (BNP) (C) in these rats at the end of the 7-day drug treatments. Values for post-MI rats receiving AdGFP in their adrenals instead of Adbarr1 (i.e. not overexpressing barr1 in their adrenals) were used as reference. *, p < 0.05, vs. Candesartan (Adbarr1), n=5 rat hearts/group.
S1359	Losartan Potassium (DuP 753) Losartan is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.	Antiviral Res, 2015, 120:140-6 Sci Rep, 2015, 5:8116	Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.
S1738	Telmisartan Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.	Sci Rep, 2015, 5:8116	(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan.
S4975^新	Fimasartan Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) with noncompetitive, insurmountable binding with the AT1 receptor. It is used for the treatment of hypertension and heart failure.
S1507	Irbesartan Irbesartan (SR-47436, BMS-186295) is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.	Antiviral Res, 2015, 120:140-6 Sci Rep, 2015, 5:8116	Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p <0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.
S1894	Valsartan Valsartan is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.	J Nat Med, 2014, 68(3):623-9 Sci Rep, 2015, 5:8116	Effect of valsartan and cardamonin on Ang II-induced phosphorylation of p38 MAPK and ERK. Representative results of Western blot.
S7098	PD123319 PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.	Exp Biol Med, 2015, 10.1177/1535370215576312 Naunyn Schmiedebergs Arch Pharmacol, 2016, 389(12):1333-1340 Acta Biochim Biophys Sin, 2015, 47(7), 1–9	Effect of PD123319 treatment on sodium current (INa). Typical recordings of INa in cells from control (a), non-PD123319 (b), and PD123319 (c). x-axis: time (ms mini-second); y-axis: current volume (pA). The voltage clamp protocol is shown in (d). e Average I-V relationships of INa density (pA/pF) as a function of step potential (mV), obtained in control (filled squares), non-PD123319 (empty squares), and PD123319 (empty circles)
S1604	Olmesartan Medoxomil Olmesartan Medoxomil (CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.	Sci Rep, 2015, 5:8116	Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 mM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A–B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.
S2037	Candesartan Cilexetil Candesartan Cilexetil is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.	Exp Biol Med, 2015, 10.1177/1535370215576312 Sci Rep, 2015, 5:8116	(b) ASMCs were incubated with 1 µM candesartan or 10 µM PD123319 for 60 min before stimulation with 0.1 µM Ang II for 24 h in six-well plates. Western blot was used for analyses of the levels of MMP-2 expression in cell lysates. Top panel: Graphs show the relative MMP-2 protein levels normalized to GAPDH relative to control. Bottom panel: Ratio of MMP-2/GAPDH protein expression from a representative Western blot experiment. Shown are mean ± SEM of three individual experiments. **P < 0.01 vs. untreated control cells; ##P < 0.01 vs. cells treated with Ang II
S3057	Azilsartan Medoxomil Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.	Sci Rep, 2015, 5:8116	(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.
S3046	Azilsartan Azilsartan is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM.	Sci Rep, 2015, 5:8116	(B) Dose-response curves of each drug for acute G protein or βarr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.
S4102	Eprosartan Mesylate Eprosartan is a nonpeptide angiotensin II receptor antagonist, [³H]-eprosartan binds to the AT1 receptor with K_D of 0.83 nM in rat vascular smooth muscle cells.	Sci Rep, 2015, 5:8116 Sci Rep, 2016, 10.1038/srep25694	(B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.
S2199	Aliskiren Hemifumarate Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.
S1657	Enalaprilat Dihydrate Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.
S5067^新	Losartan Losartan is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement.
S5728^新	Delapril Hydrochloride
S5712^新	Zofenopril calcium Zofenopril calcium is an angiotensin-converting enzyme (ACE) inhibitor that protects the heart and helps reduce high blood pressure.
S1506	Perindopril Erbumine Perindopril Erbumine is a potent ACE inhibitor with IC50 of 1.05 nM.
S1793	Ramipril Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
S1941	Enalapril Maleate Enalapril Maleate is an angiotensin-converting enzyme (ACE) inhibitor, used in the treatment of hypertension, diabetic nephropathy, and chronic heart failure.
S2051	Captopril Captopril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 6 nM.
S2076	Lisinopril Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
S2081	Cilazapril Monohydrate Cilazapril Monohydrate is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
S2079	Moexipril HCl Moexipril HCl is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure.
S2581	Quinapril HCl Quinapril HCl is the hydrochloride salt of quinapril that is an angiotensin-converting enzyme inhibitor with a Ki of 20 μM.
S2099	Temocapril HCl Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.
S2100	Temocapril Temocapril is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.
S2109	Imidapril HCl Imidapril HCl is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 2.6 nM, used for the treatment of hypertension.
S7678	LCZ696 Sacubitril/valsartan (LCZ696), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.	J Mol Cell Cardiol, 2017, 108:138-148	Histological analysis staining of three groups. (a) Representative H&E-staining micrographs displaying transverse myocardial section (original magnification ×200). (b) Masson staining of three groups (original magnification ×200). Collagen content (%) of heart tissues were presented as fibrosis (**P < 0.001, n = 7 per group). (c) Cardiac section of three group mice hearts stained with WGA (original magnification ×400) (P < 0.05, n = 7 per group). (d) The expression of Drp1 significantly increased in DOX group (*P < 0.001, n = 7 per group) and it decreased in DOX + LCZ696 group (P < 0.01, n = 7 per group).
S2095	Fosinopril Sodium Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.

研究分野別

製品類型

RAAS

シグナル伝達経路

研究分野

亜型選択性的な製品