| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Atrial natriuretic factor (1-28) targets the natriuretic peptide receptor type A (NPR-A), a membrane-bound guanylyl cyclase receptor. Residues Phe8, Arg14, and the C-terminal sequence of ANP are known to bind to human NPR-A. Upon binding, ANP activates NPR-A, which catalyzes the conversion of GTP to cGMP, leading to vasodilation, natriuresis, and diuresis. ANP also inhibits endothelin-1 secretion in a dose-dependent manner in endothelial cells and suppresses pro-opiomelanocortin (POMC) mRNA expression in the pituitary.
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| ln Vitro |
Guanosine 3',5'-cyclic monophosphate (cGMP) is significantly increased by ANF-(1-28), rising from 1.3 +/- 0.3 to 106 +/- 22 pmol cGMP/10(6) cells [50% effective dosage (ED50) = 1.2 nM][1].
In vitro, atrial natriuretic factor (1-28) is a diuretic, natriuretic, and vasodilatory peptide hormone. In cultured porcine endothelial cells, ANP (1-28) inhibits immunoreactive endothelin-1 secretion after stimulation with Angiotensin II (Ang II) in a dose-dependent manner. This inhibition is paralleled by an increase in cGMP accumulation. ANP also suppresses POMC mRNA expression in pituitary cell cultures with a potency similar to its in vivo activity, while having only modest inhibition on betaEP-LI release. |
| ln Vivo |
Every day of the research, the ANF-(1-28) (0.5 µg/kg/min) infusion reduces the increase in plasma creatinine levels by around 50%[3].
In vivo, atrial natriuretic factor (1-28) exhibits potent blood pressure lowering activity by increasing sodium and urine excretion (natriuresis and diuresis) and inducing vasorelaxation. It plays an important role in blood pressure regulation, fluid-electrolyte homeostasis, and cardiovascular function. In heart failure models, ANP improves hemodynamics by reducing preload and afterload. ANP also suppresses renin and aldosterone secretion, contributing to its hypotensive effects. The peptide is involved in cardiac injury response and mechanical stretch sensing. |
| Enzyme Assay |
For in vitro receptor binding assays, ANP (1-28) is dissolved in an appropriate buffer (e.g., 50 mM Tris-HCl, pH 7.4, containing 5 mM MgCl2, 0.1% BSA, and protease inhibitors). Competition binding assays are performed using membrane preparations from cells expressing NPR-A (e.g., HEK293-NPR-A or native tissues). Membranes are incubated with radiolabeled ANP (e.g., ¹2⁵I-ANP, 0.05-0.1 nM) and increasing concentrations of unlabeled ANP (10-¹¹-10-⁶ M) at 4degC for 2-24 hours. Bound and free radioligands are separated by rapid filtration through GF/B filters pre-soaked in 0.3% polyethyleneimine. Filters are washed and counted. Kd and Ki values are calculated. For cGMP assays, cells expressing NPR-A are treated with ANP (0.1 nM-1 uM) for 5-30 minutes, and intracellular cGMP is measured by ELISA or radioimmunoassay.
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| Cell Assay |
For cell-based studies, cells expressing NPR-A (e.g., endothelial cells, vascular smooth muscle cells, HEK293-NPR-A transfectants) are cultured in standard medium (DMEM with 10% FBS, 1% penicillin-streptomycin) at 37degC with 5% CO2. Cells are seeded in 6- or 96-well plates at appropriate densities. For cGMP assays, cells are pre-incubated with 0.5 mM 3-isobutyl-1-methylxanthine (IBMX, a phosphodiesterase inhibitor) for 10-30 minutes, then treated with ANP (0.1 nM-1 uM) for 5-30 minutes. The reaction is stopped by removing the medium and adding 0.1 M HCl. cGMP levels in cell lysates are quantified by ELISA or radioimmunoassay. For endothelin-1 inhibition assays, porcine endothelial cells are stimulated with Angiotensin II (100 nM) in the presence or absence of ANP (0.1-100 nM) for 4-24 hours, and endothelin-1 levels in culture supernatants are measured by ELISA. For POMC mRNA suppression studies, pituitary cell cultures are treated with ANP (1-100 nM) and POMC mRNA is quantified by qPCR.
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| Animal Protocol |
For in vivo studies, ANP (1-28) (Carperitide) is typically administered to rodents via intravenous infusion (bolus injection or continuous infusion). A typical protocol for blood pressure studies involves intravenous administration of ANP at 0.03-0.3 ug/kg/min via a jugular vein catheter in anesthetized or conscious rats. Blood pressure and heart rate are monitored via arterial catheter. For diuresis/natriuresis studies, animals are placed in metabolic cages, and urine is collected for 30-60 minutes after ANP administration. Urine sodium and potassium concentrations are measured by flame photometry or ion-selective electrodes. For heart failure models (e.g., rat coronary ligation or dog rapid ventricular pacing), ANP is infused intravenously and hemodynamic parameters are measured using a Swan-Ganz catheter or pressure-volume loop analysis. In clinical use, Carperitide is administered intravenously as a bolus followed by continuous infusion (typically 0.1-0.2 ug/kg/min) to treat acute heart failure.
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| ADME/Pharmacokinetics |
Atrial natriuretic factor (1-28) has a relatively large apparent volume of distribution (averaging 30 +/- 5 L in humans) and a short half-life of 4.7 +/- 0.7 minutes (following 50 ug) and 10.7 +/- 3.8 minutes (following 100 ug). It is cleared primarily by the natriuretic peptide clearance receptors (NPR-C) and neutral endopeptidase (NEP, neprilysin), which degrade the peptide. In patients with severe heart failure, ANP pharmacokinetics are altered, and the half-life may be prolonged. Clearance is reduced in renal failure. The short half-life necessitates continuous infusion for therapeutic use.
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| Toxicity/Toxicokinetics |
Atrial natriuretic factor is an endogenous peptide hormone and has been extensively studied in clinical trials for safety. At lower infusion rates (0.03-0.2 ug/kg/min), ANP is generally well-tolerated. At higher infusion rates (>0.45 ug/kg/min), adverse reactions including bradycardia and hypotension may occur. Prolonged infusion in sodium-depleted subjects can cause symptomatic hypotension. No significant organ toxicity has been reported at therapeutic doses. As a research peptide, standard laboratory precautions for handling biological agents apply. Not for human consumption except for pharmaceutical formulations.
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| References |
[1]. B M Fontoura, et al. Atrial natriuretic factor receptors in cultured renomedullary interstitial cells. Am J Physiol. 1990 Apr;258(4 Pt 1):C692-9.
[2]. T T Tan, et al. ANF(1-28) is a potent suppressor of pro-opiomelanocortin (POMC) mRNA but a weak inhibitor of beta EP-LI release from AtT-20 cells. J Endocrinol. 1994 Nov;143(2):R1-4. [3]. D M Pollock, et al. Beneficial effect of the ANF analog A68828 on recovery from ischemic acute renal failure. Ren Fail. 1992;14(2):141-6. |
| Additional Infomation |
Atrial natriuretic factor (1-28), human, porcine is also known as Carperitide. Carperitide is an approved drug for the treatment of acute decompensated heart failure in Japan and has been used clinically since 1995. It is administered intravenously and is indicated for patients with acute heart failure to improve hemodynamics, reduce preload and afterload, and promote natriuresis. Numerous clinical trials have evaluated ANP for acute heart failure (e.g., the J-WIND study, PROTECT trial, TRUE-AHF trial). Studies have also investigated ANP for acute renal failure, oliguric acute tubular necrosis, and pulmonary hypertension. Carperitide has been evaluated in Phase 2 and Phase 3 clinical trials, with some studies showing reduced need for dialysis in oliguric acute renal failure. For research use only; clinical use requires pharmaceutical-grade Carperitide.
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| Molecular Formula |
C127H205N45O39S3
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|---|---|
| Molecular Weight |
3080.46
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| Exact Mass |
3078.44
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| CAS # |
91917-63-4
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| PubChem CID |
16133394
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
55
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| Hydrogen Bond Acceptor Count |
48
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| Rotatable Bond Count |
109
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| Heavy Atom Count |
214
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| Complexity |
6900
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)CC1C=CC=CC=1)(C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(=O)O)CC1C=CC(O)=CC=1)CC1C=CC=CC=1
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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 | 0.3246 mL | 1.6231 mL | 3.2463 mL | |
| 5 mM | 0.0649 mL | 0.3246 mL | 0.6493 mL | |
| 10 mM | 0.0325 mL | 0.1623 mL | 0.3246 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.
Products are for research use only; We do not sell to patients
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