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| Targets |
C-Type Natriuretic Peptide (1-53), human TFA primarily acts through the natriuretic peptide receptor-B (NPR-B), also known as NPR2, which is a guanylyl cyclase receptor. Binding of CNP to NPR-B leads to intracellular cGMP production, promoting vasodilation, reducing blood pressure, and exerting anti-fibrotic effects in cardiac and renal fibroblasts. It may also bind to the clearance receptor NPR3.
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| ln Vitro |
In vitro, CNP (1-53) activates particulate guanylyl cyclase B (pGC-B/NPR-B) in vascular smooth muscle cells, raising intracellular cGMP levels. The native CNP induces cGMP production, and the elongated form CNP-53 is processed to CNP-22. The CNPs share considerable sequence homology with ANP and BNP within the disulfide loop and exert similar pharmacological actions, albeit with different relative potencies.
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| ln Vivo |
In vivo, CNP (1-53) is used in research to explore its therapeutic potential in cardiovascular diseases, particularly in conditions like heart failure and hypertension. It promotes vasodilation and reduces blood pressure through the NPR-B/cGMP pathway. CNP and its analogs (e.g., C53, a CNP analog) exhibit sustained in vivo activity with anti-fibrotic actions in human cardiac and renal fibroblasts. CNP-53 is the N-terminally elongated form found in brain and tissues.
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| Enzyme Assay |
For in vitro enzyme-binding assays (non-cell-based), binding of CNP to NPR-B is typically assessed by measuring cGMP production in membrane preparations. Membranes from NPR-B-expressing cells (e.g., vascular smooth muscle cells or HEK293 cells overexpressing NPR-B) are prepared by homogenization and centrifugation. The membrane fraction (10-50 microg protein) is incubated with varying concentrations of CNP (1-53) (0-1000 nM) in assay buffer containing 0.5 mM 3-isobutyl-1-methylxanthine (IBMX, phosphodiesterase inhibitor) and an ATP-regenerating system (e.g., 1 mM ATP, 5 mM creatine phosphate, 100 U/mL creatine phosphokinase) in a final volume of 100 microL. After incubation at 37degC for 15-30 minutes, the reaction is terminated by adding 50 microL of 0.1 M HCl. cGMP accumulation is measured by enzyme immunoassay (EIA) or radioimmunoassay (RIA) using a commercial kit. The EC50 value is calculated from the dose-response curve. Binding affinity to NPR3 (clearance receptor) can be measured by radioligand binding assays using [¹2⁵I]-CNP as the tracer and membranes from NPR3-expressing cells, as described in the literature (PubMed ID: 11533490).
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| Cell Assay |
For cell-based assays, primary human cardiac fibroblasts (HCFs) or renal fibroblasts (HRFs) are cultured in 6- or 12-well plates. When cells reach 70-80% confluence, they are serum-starved for 4-6 hours and then treated with CNP (1-53) (0-1000 nM) in the presence of 0.5 mM IBMX for 15-30 minutes at 37degC. After treatment, cells are lysed in 0.1 M HCl, and the lysate is collected. cGMP levels in the lysate are measured by EIA or RIA. For anti-fibrotic activity assays, fibroblasts are treated with transforming growth factor-beta (TGF-beta, 1-10 ng/mL) in the presence or absence of CNP (1-53) (0-1000 nM) for 24-48 hours. RNA is extracted, and expression of fibrotic markers (collagen I, alpha-SMA, fibronectin) is measured by qRT-PCR. Alternatively, cells are fixed and stained for alpha-SMA to assess myofibroblast differentiation. Cell viability and cytotoxicity are assessed using MTT or LDH assays to ensure CNP does not cause non-specific toxicity. For vascular relaxation assays, isolated rat aortic rings are mounted in a myograph, precontracted with phenylephrine (1 microM), and treated with CNP (1-53) to assess endothelium-independent vasodilation via NPR-B on vascular smooth muscle cells.
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| Animal Protocol |
For in vivo animal studies, C-Type Natriuretic Peptide (1-53), human TFA is typically administered intravenously or by subcutaneous injection to rodents (rats or mice). For blood pressure studies, male Sprague-Dawley rats (250-350 g) are anesthetized with isoflurane, and a catheter is inserted into the carotid artery for blood pressure monitoring. CNP (1-53) is administered as a bolus injection (e.g., 1-100 microg/kg in 100-200 microL saline) via a jugular vein catheter. Mean arterial pressure (MAP) and heart rate are recorded continuously for up to 60 minutes post-injection. For anti-fibrosis studies, a mouse model of renal or cardiac fibrosis is used (e.g., unilateral ureteral obstruction (UUO) or angiotensin II infusion model). CNP (1-53) is administered daily via subcutaneous injection (e.g., 50-200 microg/kg/day for 2-4 weeks). At the end of the treatment period, mice are euthanized, and tissues (kidney, heart) are collected for histological analysis (Masson's trichrome staining for collagen) and for measurement of hydroxyproline content as a marker of collagen deposition. For pharmacokinetic studies, blood samples are collected at various time points (e.g., 0, 5, 15, 30, 60, 120 minutes) after intravenous administration, and plasma CNP levels are measured by ELISA or LC-MS/MS. The TFA salt form enhances solubility for in vivo administration.
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| ADME/Pharmacokinetics |
C-Type Natriuretic Peptide (1-53), human TFA has a molecular weight of 5801.77 Da. The peptide sequence is: Asp-Leu-Arg-Val-Asp-Thr-Lys-Ser-Arg-Ala-Ala-Trp-Ala-Arg-Leu-Leu-Gln-Glu-His-Pro-Asn-Ala-Arg-Lys-Tyr-Lys-Gly-Ala-Asn-Lys-Lys-Gly-Leu-Ser-Lys-Gly-Cys-Phe-Gly-Leu-Lys-Leu-Asp-Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu-Gly-Cys (disulfide bridge: Cys37-Cys55). The TFA salt is the trifluoroacetate form, which enhances water solubility and is commonly used for peptide handling. Peptide purity is typically ≥95% by HPLC. The product is supplied as a lyophilized powder. Storage: protect from moisture; store at -20degC for up to 3 years; in solution at -80degC for up to 1 year. Solubility: H2O (soluble); the TFA salt promotes solubility in aqueous buffers. For in vivo administration, the peptide is typically reconstituted in sterile 0.9% saline or PBS at concentrations of 0.1-1 mg/mL and used immediately. Avoid repeated freeze-thaw cycles. CNP is susceptible to enzymatic degradation by neutral endopeptidase (NEP); for prolonged in vivo exposure, NEP inhibitors may be co-administered or stabilized analogs (e.g., C53) may be used.
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| Toxicity/Toxicokinetics |
C-Type Natriuretic Peptide (1-53), human TFA is a research-grade peptide for laboratory use only. It is not for human therapeutic or diagnostic use. At typical research doses (microg/kg range in animals), CNP is generally well-tolerated. High doses may cause hypotension, which is expected due to its vasodilatory effect. Standard safety monitoring (body weight, behavior, blood pressure, hematological parameters) should be performed. As a research peptide, no extensive toxicology data are available; standard precautions for handling peptides (gloves, lab coat, eye protection) should be followed. The TFA salt is considered relatively non-toxic at the concentrations used in research.
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| References | |
| Additional Infomation |
C-Type Natriuretic Peptide (1-53), human TFA (CNP-53, CAS 141294-77-1) is the full-length form of C-type natriuretic peptide, which is processed to the active CNP-22. CNP-53 is a major storage form in tissues and is converted to CNP-22 by proteolytic processing. CNP has important roles in cardiovascular homeostasis, bone growth (achondroplasia regulation), and reproductive function. The peptide is used in research for studying hypertension, heart failure, renal fibrosis, and skeletal disorders. It is supplied as a TFA salt (trifluoroacetate) to improve solubility. The product is for research use only and is not approved for clinical use. Citations: identified in porcine brain (Biochem Biophys Res Commun. 1990 Jul 31;170(2):973-9).
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| Molecular Formula |
C251H417N81O71S3.C2HF3O2
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| Molecular Weight |
5915.79
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| Related CAS # |
C-Type Natriuretic Peptide (1-53), human;141294-77-1
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| Appearance |
Solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 0.1690 mL | 0.8452 mL | 1.6904 mL | |
| 5 mM | 0.0338 mL | 0.1690 mL | 0.3381 mL | |
| 10 mM | 0.0169 mL | 0.0845 mL | 0.1690 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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