Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension[1][3][6].
LCZ696 is a dual angiotensin II receptor and neprilysin inhibitor.
Olmesartan methyl ester is an intermediate in the synthesis of Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor antagonist with IC50 of 66.2 μM[1][2].
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Irbesartan D4 is the deuterium labeled Irbesartan, which is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist.
Valsartan (CGP-48933) is an angiotensin II receptor antagonist for treatment of high blood pressure and heart failure.
Trans-Tranilast is an antiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.Target: Angiotensin ReceptorTranilast has been approved in Japan and South Korea, since 1982, for the treatment of bronchial asthma, with indications for keloids and hypertrophic scar added in 1993. Tranilast is also used to treat asthma, autoimmune diseases, atopic and fibrotic pathologies, and can also inhibit angiogenesis. The antiproliferative properties of tranilast were found that tranilast elicited an inhibitory effect on fibroblast proliferation in vitro and also suppressed collagen production both in vitro and in vivo . Tranilast also reduced the release of chemical mediators from mast cells and suppressed hypersensitivity reactions. [1]Three-week-old C57Bl/10 and mdx mice received tranilast (~300 mg/kg) in their food for 9 weeks, after which fibrosis was assessed through histological analyses, and functional properties of tibialis anterior muscles were assessed in situ and diaphragm muscle strips in vitro. Tranilast administration did not significantly alter the mass of any muscles in control or mdx mice, but it decreased fibrosis in the severely affected diaphragm muscle by 31% compared with untreated mdx mice (P< 0.05) [2].
Valsartan Ethyl Ester is an impurity of Valsartan. Valsartan is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure[1].
Angiotensin II 5-valine is an agonist of angiotensin receptor.
Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor[1].
Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension[1][3][6].
ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.IC50 value:Target: AT2 R agonistin vitro: CGP42112 (>==1 nM) significantly inhibited cGMP production from the basal value. CGP42112 (>==1 nM) significantly inhibited TH-enzyme activity from the basal value. These inhibitory effects of CGP42112 on TH-enzyme activity and-cGMP production were abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) was ineffective [1]. [125I]CGP 42112 bound selectively to the AT2 angiotensin II receptor subtype. [125I]CGP 42112 bound with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP 42112 binding in the brain, but did not alter its binding in the adrenal [2]. [125I]CGP 42112 bound with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP 42112 binding was selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP 42112 and the non-selective peptides Ang II and angiotensin III (Ang III) [4].in vivo: Intravenous infusions of CGP 42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF [3].
Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM [2]Target: AT1 receptorin vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors[1].in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively [2]. Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan[3]. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide [4].
Tranilast is an antiallergic agent.Target: Angiotensin ReceptorTranilast has been approved in Japan and South Korea, since 1982, for the treatment of bronchial asthma, with indications for keloids and hypertrophic scar added in 1993. Tranilast is also used to treat asthma, autoimmune diseases, atopic and fibrotic pathologies, and can also inhibit angiogenesis. The antiproliferative properties of tranilast were found that tranilast elicited an inhibitory effect on fibroblast proliferation in vitro and also suppressed collagen production both in vitro and in vivo . Tranilast also reduced the release of chemical mediators from mast cells and suppressed hypersensitivity reactions. [1]Three-week-old C57Bl/10 and mdx mice received tranilast (~300 mg/kg) in their food for 9 weeks, after which fibrosis was assessed through histological analyses, and functional properties of tibialis anterior muscles were assessed in situ and diaphragm muscle strips in vitro. Tranilast administration did not significantly alter the mass of any muscles in control or mdx mice, but it decreased fibrosis in the severely affected diaphragm muscle by 31% compared with untreated mdx mice (P< 0.05) [2].
Olmesartan D4 is the deuterium labeled Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
FK-739 (free base) is an angiotensin II type 1 (AT1) receptor antagonist used in the study of hypertension[1].
Angiotensin amide ((Asn1,Val5)-Angiotensin II) is a potent vasoconstrictor. Angiotensin amide is a derivative of angiotensin II. Angiotensin amide can be used as a cardiac stimulant[1].
Dehydro Olmesartan is a derivative of Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist and has the potential for high blood pressure study[1][2].
L162441 is an Angiotensin type 1 receptor antagonist.
Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons[1][2][3][4].
Candesartan D4 is the deuterium labeled Candesartan, which is an angiotensin II receptor antagonist.
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists[1].
Angiotensinogen (1-13) (human) is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides[1][2].
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
Valsartan-d3 is the deuterium labeled Valsartan[1]. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[2].
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common drug-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes[1].