| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 1g | |||
| Other Sizes |
| Targets |
MCUF-651 targets guanylyl cyclase A receptor (GC-A), the receptor for atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP). It is a positive allosteric modulator (PAM) of GC-A with an EC50 of 0.45 μM and a KD of 397 nM. By binding to GC-A, MCUF-651 selectively enhances the binding of ANP to GC-A and increases ANP-mediated cGMP production, leading to vasodilation, natriuresis, and inhibition of cardiomyocyte hypertrophy.
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| ln Vitro |
In vitro, MCUF-651 enhances ANP-mediated cGMP generation in human cardiac, renal, and fat cells. It inhibits cardiomyocyte hypertrophy, demonstrating its cardioprotective effects. Binding analysis confirms that MCUF-651 binds to GC-A and selectively enhances the binding of ANP to GC-A. These in vitro properties make MCUF-651 a valuable tool for studying natriuretic peptide signaling and cardiovascular function.
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| ln Vivo |
In vivo, MCUF-651 is an orally active GC-A positive allosteric modulator. Its ability to enhance ANP-mediated cGMP generation suggests potential for treating cardiovascular diseases such as heart failure and hypertension. However, detailed in vivo efficacy data are limited in publicly available sources. The compound's oral bioavailability makes it suitable for in vivo studies.
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| Enzyme Assay |
The in vitro receptor binding assay for MCUF-651 involves measuring its binding affinity to GC-A. The compound is incubated with recombinant GC-A or cell membranes expressing GC-A in the presence of a labeled ligand (e.g., radiolabeled ANP or a fluorescent ANP analog). Binding affinity (KD) is determined using saturation or competition binding assays. The positive allosteric modulation can be assessed by measuring ANP binding in the presence of MCUF-651.
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| Cell Assay |
The in vitro cell-based assay for MCUF-651 involves culturing human cardiac, renal, or fat cells and treating them with the compound to assess effects on cGMP production and cellular function. Cells are treated with MCUF-651 at various concentrations, with or without ANP stimulation. cGMP levels are measured using ELISA or radioimmunoassay. Cardiomyocyte hypertrophy is assessed by measuring cell size, protein content, or expression of hypertrophy markers (e.g., ANP, BNP, β-MHC) in cardiomyocytes treated with hypertrophic stimuli in the presence or absence of MCUF-651.
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| Animal Protocol |
In vivo animal studies for MCUF-651 have not been extensively reported. If conducted, such studies might involve mouse or rat models of heart failure or hypertension. MCUF-651 would be administered orally at various doses, and blood pressure, cardiac function, and natriuretic peptide signaling would be assessed. Standard protocols for cardiovascular disease models would be employed. No specific data are available.
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| ADME/Pharmacokinetics |
MCUF-651 is an orally active small molecule with favorable pharmacokinetic properties. It has a molecular weight of 368.44 and a molecular formula of C17H22F2N4OS. The compound is a positive allosteric modulator of GC-A with an EC50 of 0.45 μM and a KD of 397 nM. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources but are expected to be characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of MCUF-651 has not been systematically evaluated. As a GC-A positive allosteric modulator that enhances natriuretic peptide signaling, its primary safety concerns would relate to hypotension and electrolyte imbalances. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
MCUF-651 is a research compound and has not been approved for clinical use. It is an orally active positive allosteric modulator of GC-A with an EC50 of 0.45 μM and a KD of 397 nM. MCUF-651 enhances ANP-mediated cGMP generation in human cardiac, renal, and fat cells and inhibits cardiomyocyte hypertrophy. It is a valuable tool for studying natriuretic peptide signaling and cardiovascular diseases.
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| Molecular Formula |
C17H22F2N4OS
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|---|---|
| Molecular Weight |
368.444589138031
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| Exact Mass |
368.15
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| Elemental Analysis |
C, 55.42; H, 6.02; F, 10.31; N, 15.21; O, 4.34; S, 8.70
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| CAS # |
2747162-85-0
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| PubChem CID |
162345705
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| Appearance |
White to off-white solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
470
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCN1CCCC(C1)C(=O)NC2=NC3=C(C=C(C=C3S2)F)F
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| InChi Key |
NOPAIELWJAFUCL-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-(4,6-difluorobenzo[d]thiazol-2-yl)-1-(2-(dimethylamino)ethyl)piperidine-3-carboxamide
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| Synonyms |
MCUF-651; MCUF 651 MCUF651;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7141 mL | 13.5707 mL | 27.1415 mL | |
| 5 mM | 0.5428 mL | 2.7141 mL | 5.4283 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7141 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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