Structure
Omapatrilat, Inhibitor
Omapatrilat
Purity
98.00%
Synonyms
Omapatrilat; BMS-186716; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 31mg/mL (75.88mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C19H24N2O4S2
SMILES
O=C([C@@H]1CCC[C@](N21)([H])SCC[C@H](NC([C@@H](S)CC3=CC=CC=C3)=O)C2=O)O
CAS Number
167305-00-2
Target & IC50
NEP: ic50 0.45nM (ki)
ACE: ic50 0.64nM (ki)
ACE: ic50 0.64nM (ki)
In Vitro
In vitro autoradiography using the specific NEP inhibitor radioligand 125I-RB104 and the specific ACE inhibitor radioligand 125I-MK351A display omapatril at (10mg/kg) induces rapid and effective inhibition of renal NEP and ACE, respectively, for 24 hours. Omapatrilat displays high potency for NEP, NEP2 and ACE, moderate strong activity against APP, but low activity against ECE1 (Ki=0.45, 25, 0.64, 250nM) [1][4].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Omapatrilat, inhibitor
Omapatrilat is a metalloprotease ACE and NEP dual inhibitor (Ki: 0.64 and 0.45nM, respectively).
Product Categories/Family for Omapatrilat, inhibitor
References
Fryer RM, et al. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy ofenzymes associated with bradykinin-mediated angioedema. Br J Pharmacol. 2008 Mar;153(5):947-55.
Fryer RM, et al. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy ofenzymes associated with bradykinin-mediated angioedema. Br J Pharmacol. 2008 Mar;153(5):947-55.
Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7.
Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7.
Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6.
Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6.
Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6.
Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6.
Fryer RM, et al. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy ofenzymes associated with bradykinin-mediated angioedema. Br J Pharmacol. 2008 Mar;153(5):947-55.
Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7.
Robl JA, et al. Dual metalloprotease inhibitors: mercaptoacetyl-based fused heterocyclic dipeptide mimetics asinhibitors of angiotensin-converting enzyme and neutral endopeptidase. J Med Chem. 1997 May 23;40(11):1570-7.
Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6.
Ichiki T, et al. Endothelial permeability in vitro and in vivo: protective actions of ANP and omapatrilat in experimental atherosclerosis. Peptides. 2013 Oct;48:21-6.
Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6.
Burrell LM, et al. Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6.
Similar Products
Product Notes
The Omapatrilat (Catalog #AAA5755303) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Omapatrilat, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
If you are ready to order, navigate to Shopping Cart and get ready to checkout.
