| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
sGC[1][2]
Soluble guanylate cyclase (sGC). CFM 1571 acts as a stimulator of sGC, the primary receptor for nitric oxide (NO). This activation leads to increased conversion of GTP to cGMP, a key second messenger in cardiovascular and neurological signaling. |
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| ln Vitro |
In a cell-free enzyme assay, CFM 1571 activates sGC with an EC50 of 5.49 microM. It also inhibits collagen-stimulated platelet aggregation in vitro with an IC50 of 2.84 microM, demonstrating functional effects downstream of sGC activation.
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| ln Vivo |
Pharmacokinetic studies in rats indicate that CFM 1571 exhibits modest oral bioavailability (12%). It shows no significant inhibition of phosphodiesterases or nitric oxide synthases, suggesting a favorable selectivity profile for studying sGC-specific effects in vivo.
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| Enzyme Assay |
A cell-free assay is performed using purified recombinant human sGC enzyme. The enzyme is incubated in a reaction buffer containing GTP and varying concentrations of CFM 1571. After a defined period, the reaction is stopped, and the amount of cGMP produced is quantified using a competitive ELISA or a luminescence-based method. The EC50 (5.49 microM) is calculated as the concentration required to produce half-maximal cGMP production.
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| Cell Assay |
For cellular assays, rat or human platelets are isolated and pre-incubated with varying concentrations of CFM 1571. Platelet aggregation is stimulated by the addition of collagen. Aggregation is monitored using a light transmission aggregometer. The IC50 (2.84 microM) is the concentration that reduces maximal aggregation by 50%, confirming the compound‘s anti-platelet effect via sGC activation.
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| Animal Protocol |
Pharmacokinetic studies are performed in male Sprague-Dawley rats. CFM 1571 hydrochloride is administered via both intravenous (IV) and oral (PO) routes. Blood samples are collected at multiple time points post-dose, and plasma concentrations are analyzed by LC-MS/MS. The oral bioavailability is calculated as 12%, along with other PK parameters like Cmax, Tmax, and half-life.
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| ADME/Pharmacokinetics |
Following oral administration, CFM 1571 exhibits modest oral bioavailability (12%) in rats, indicating that it is systemically available but may undergo first-pass metabolism. No other specific PK parameters (e.g., Cmax, Tmax, half-life) have been reported, but its bioavailability makes it suitable for in vivo studies.
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| Toxicity/Toxicokinetics |
Not reported. No formal toxicology data is available for CFM 1571 hydrochloride as it is a research tool. However, off-target profiling shows it has no significant inhibition of phosphodiesterases or nitric oxide synthases (iNOS 25%, nNOS 17%), suggesting a low risk of off-target toxicity related to these enzyme families.
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| References |
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| Additional Infomation |
CFM 1571 is a sGC stimulator that acts independently of NO, similar to clinical drugs like riociguat (used for pulmonary hypertension) and vericiguat (for heart failure). Its selectivity for sGC over adenylyl cyclase and other off-targets makes it a valuable research tool. The compound's modest oral bioavailability (12%) and ability to inhibit platelet aggregation highlight its potential for studying thrombotic disorders and sGC biology in the cardiovascular system.
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| Molecular Formula |
C23H29CLN4O3
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|---|---|
| Molecular Weight |
444.95
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| Exact Mass |
444.192
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| CAS # |
1215548-30-3
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| PubChem CID |
56972190
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
31
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| Complexity |
505
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCCOC1=NN(C(=C1)C(=O)NC2=CC=C(C=C2)OC)CC3=CC=CC=C3.Cl
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| InChi Key |
DFVHCFCSCUCAPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N4O3.ClH/c1-26(2)14-7-15-30-22-16-21(27(25-22)17-18-8-5-4-6-9-18)23(28)24-19-10-12-20(29-3)13-11-19;/h4-6,8-13,16H,7,14-15,17H2,1-3H3,(H,24,28);1H
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| Chemical Name |
1-benzyl-3-[3-(dimethylamino)propoxy]-N-(4-methoxyphenyl)pyrazole-5-carboxamide;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 100 mg/mL (224.74 mM)
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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 | 2.2474 mL | 11.2372 mL | 22.4744 mL | |
| 5 mM | 0.4495 mL | 2.2474 mL | 4.4949 mL | |
| 10 mM | 0.2247 mL | 1.1237 mL | 2.2474 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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