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MedKoo Cat#: 556203 | Name: MCUF-651
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

MCUF-651
MCUF-651
CAS#2747162-85-0

Theoretical Analysis

MedKoo Cat#: 556203

Name: MCUF-651

CAS#: 2747162-85-0

Chemical Formula: C17H22F2N4OS

Exact Mass: 368.1482

Molecular Weight: 368.45

Elemental Analysis: C, 55.42; H, 6.02; F, 10.31; N, 15.21; O, 4.34; S, 8.70

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to Ship
10mg USD 250.00 Ready to Ship
25mg USD 450.00 Ready to Ship
50mg USD 750.00 Ready to Ship
200mg USD 1,950.00 Ready to Ship
1g USD 4,650.00 Ready to Ship
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Related CAS #
No Data
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
More Info
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
Biological target:
MCUF-651 is a small molecule guanylyl cyclase A receptor positive allosteric modulator (GC-A PAM).
In vitro activity:
From the aforementioned hit to lead efforts, this study identified MCUF-651 as the lead selective GC-A PAM, as it was able to potentiate ANP-mediated cGMP (Fig. 3 A and B) and with a potency of EC50 = 0.45 µM in HEK293 GC-A cells. Thus, MCUF-651 was specific for GC-A and stimulated cGMP generation in a dose-dependent fashion only in PAM mode. Increasing concentrations of MCUF-651 shifted the ANP-mediated cGMP dose–response curve to the left (or greater potencies), with no effect on maximal ANP concentration, indicating a PAM without agonist activity. Reference: Proc Natl Acad Sci U S A. 2021 Dec 28;118(52):e2109386118. https://pubmed.ncbi.nlm.nih.gov/34930837/
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 368.45 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.

Recalculate based on batch purity %
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
Formulation protocol:
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.
In vitro protocol:
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.
In vivo protocol:
TBD
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.