WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H556203
Description: MCUF-651 is a small molecule guanylyl cyclase A receptor positive allosteric modulator (GC-A PAM). MCUF-651 enhanced ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibited cardiomyocyte hypertrophy in vitro. Further, binding analysis confirmed MCUF-651 binds to GC-A and selectively enhances the binding of ANP to GC-A. Moreover, MCUF-651 is orally bioavailable in mice and enhances the ability of endogenous ANP and BNP, found in the plasma of normal subjects and patients with hypertension or heart failure, to generate GC-A-mediated cGMP ex vivo.
Hodoodo Cat#: H556203
Chemical Formula: C17H22F2N4OS
Exact Mass: 368.1482
Molecular Weight: 368.4468
Elemental Analysis: C, 55.42; H, 6.02; F, 10.31; N, 15.21; O, 4.34; S, 8.70
Synonym: MCUF-651; MCUF 651 MCUF651;
IUPAC/Chemical Name: N-(4,6-difluorobenzo[d]thiazol-2-yl)-1-(2-(dimethylamino)ethyl)piperidine-3-carboxamide
InChi Key: NOPAIELWJAFUCL-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H22F2N4OS/c1-22(2)6-7-23-5-3-4-11(10-23)16(24)21-17-20-15-13(19)8-12(18)9-14(15)25-17/h8-9,11H,3-7,10H2,1-2H3,(H,20,21,24)
SMILES Code: O=C(C1CN(CCN(C)C)CCC1)NC2=NC3=C(F)C=C(F)C=C3S2
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 368.4468 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Sangaralingham SJ, Kuhn M, Cannone V, Chen HH, Burnett JC. Natriuretic peptide pathways in heart failure: further therapeutic possibilities. Cardiovasc Res. 2023 Feb 3;118(18):3416-3433. doi: 10.1093/cvr/cvac125. PMID: 36004816; PMCID: PMC9897690.
2: Sangaralingham SJ, Whig K, Peddibhotla S, Kirby RJ, Sessions HE, Maloney PR, Hershberger PM, Mose-Yates H, Hood BL, Vasile S, Pan S, Zheng Y, Malany S, Burnett JC Jr. Discovery of small molecule guanylyl cyclase A receptor positive allosteric modulators. Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118. doi: 10.1073/pnas.2109386118. PMID: 34930837; PMCID: PMC8719854.
The particulate guanylyl cyclase A receptor (GC-A), via activation by its endogenous ligands atrial natriuretic peptide (ANP) and b-type natriuretic peptide (BNP), possesses beneficial biological properties such as blood pressure regulation, natriuresis, suppression of adverse remodeling, inhibition of the renin-angiotensin-aldosterone system, and favorable metabolic actions through the generation of its second messenger cyclic guanosine monophosphate (cGMP). Thus, the GC-A represents an important molecular therapeutic target for cardiovascular disease and its associated risk factors. However, a small molecule that is orally bioavailable and directly targets the GC-A to potentiate cGMP has yet to be discovered