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C-Type Natriuretic Peptide (CNP) (1-22), human TFA

Alias: C-Type Natriuretic Peptide (CNP) (1-22), human TFA; 1966153-17-2; orb1691348; PD078938; glycyl-L-leucyl-L-seryl-L-lysylglycyl-L-cysteinyl-L-phenylalanylglycyl-L-leucyl-L-lysyl-L-leucyl-L-alpha-aspartyl-L-arginyl-L-isoleucylglycyl-L-seryl-L-methionyl-L-serylglycyl-L-leucylglycyl-L-cysteinecyclic(6-->22)-disulfide,trifluoroacetatesalt
Cat No.:V64214 Purity: ≥98%
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA), the 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist.
C-Type Natriuretic Peptide (CNP) (1-22), human TFA
C-Type Natriuretic Peptide (CNP) (1-22), human TFA Chemical Structure CAS No.: 1966153-17-2
Product category: Peptides
This product is for research use only, not for human use. We do not sell to patients.
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1mg
5mg
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Other Forms of C-Type Natriuretic Peptide (CNP) (1-22), human TFA:

  • C-Type Natriuretic Peptide (CNP) (1-22), human
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Product Description
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA), the 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelium-derived relaxant and growth inhibitory factor.
C-Type Natriuretic Peptide (CNP) (1-22), human TFA is an endogenous bioactive peptide corresponding to the N-terminal 1-22 amino acid fragment of human C-type natriuretic peptide. Its molecular formula is C₉₅H₁₅₈F₃N₂₇O₃₀S₃ with a molecular weight of approximately 2311.62 g/mol. This compound is the active fragment of human CNP, retaining the biological functions of the full-length peptide, and is for research use only, not intended for human or veterinary use.
Biological Activity I Assay Protocols (From Reference)
Targets
NPR-B; C-Type Natriuretic Peptide (CNP) (1-22), human TFA is a selective agonist of natriuretic peptide receptor B. It exhibits Kd values of 7 pM for NPR-B and 10.8 pM for natriuretic peptide receptor C. The compound also acts as an endogenous peptide agonist for NPR2 (NPR-B) and shows affinity for NPR3 (NPR-C). In the renal glomerulus, CNP binds to two membrane proteins: an approximately 67 kDa receptor protein with high affinity for CNP (Kd ~10⁻¹⁰ M), and an approximately 77 kDa protein with lower affinity (Kd ~10⁻⁵ M).
ln Vitro
In CHO cells expressing human NPR-B, C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) (0.01, 0.1, 1,10, 100, 1000 nM) enhances cGMP synthesis in a concentration-dependent manner[1].
In CHO cells expressing human NPR-B, C-Type Natriuretic Peptide (CNP) (1-22) (0.01-1000 nM for 15 minutes) increases cGMP production in a concentration-dependent manner. In an organ culture experiment using fetal mouse tibiae, the compound significantly promotes longitudinal bone growth. Additionally, the peptide inhibits L-type calcium currents in cardiomyocytes and exhibits antiproliferative effects in cardiac fibroblasts. CNP inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin.
ln Vivo
PK parameters of CNP immunoreactivity following a single intravenous injection of C-Type Natriuretic Peptide (CNP) (1-22), human [1]: Dose (nM/kg) AUC0-∞ (pM·min/mL) MRT0-∞ (min) T1/2 (min) CLtot (mL/min/kg) Vdss (mL/kg) 20 320±54 1.02±0.18 1.42±0.45 63.9±11.9 64.2±5.1 Subcutaneous administration of C-Type Natriuretic Peptide (CNP) (1-22), human PK parameters of post-CNP immunoreactivity: Dose (nM/kg) Cmax (pM/mL) Tmax (min) AUC0-∞ (pM·min/mL) MRT0-∞ (min) T1/2 (min) BA (%) 50 9.02±3.74 5.0±0.0 152±73 13.9±3.4 10.0±5.0 19±9. Mean residence time (MRT), total clearance (CLtot), half-life period (T1/2), and bioavailability (BA) are all defined. Humans can produce microtoxicity with C-Type Natriuretic Peptide (CNP) (1-22) at a dose of 2 nM 24 and 48 hours after application. This results in an increase in convulsion severity [3].
In conscious sheep, intravenous infusion of C-Type Natriuretic Peptide (1-22) (1 and 10 pmol·kg⁻¹·min⁻¹) exhibits natriuretic effects and reduces cardiac output by 18% without significantly affecting arterial pressure. The metabolic clearance rate of CNP is 2.48-3.15 L/min, with a rapid plasma half-life of approximately 1.6 minutes after termination of infusion. In myocardial infarction models, in vivo administration attenuates cardiac remodeling through its antifibrotic and antihypertrophic actions. In the pylorus and rectum, 2 mg/kg CNP administration markedly increases cGMP production as early as 1 minute. Intracerebroventricular administration of CNP at 2 nmol enhances the severity of picrotoxin-kindled convulsions 24 and 48 hours after application.
Enzyme Assay
Receptor binding studies in rat glomeruli are performed using ¹²⁵I-labeled Tyr⁰-CNP-(1-22). Using labeled and unlabeled ligands (CNP-(1-22), α-ANP, and C-ANP), two classes of receptor-like binding sites with different affinities for CNP are identified. Covalent attachment of ¹²⁵I-Tyr⁰-CNP-(1-22) and α-¹²⁵I-ANP identifies two membrane proteins with corresponding properties.
Cell Assay
CHO cells stably expressing human NPR-B (hNPR-B) are used to evaluate the hNPR agonist activity of test compounds. Compounds are added to cells in duplicate across a concentration range (0.01-1000 nM) and incubated for 15 minutes, after which cells are lysed. cGMP production is measured to assess receptor activation.
Animal Protocol
Conscious Sheep Study: In vehicle-controlled studies in normal conscious sheep, CNP-22 is administered intravenously at two doses (1 and 10 pmol·kg⁻¹·min⁻¹) to assess hemodynamic, renal, and hormonal effects. Rat Study: Sprague Dawley rats receive C-Type Natriuretic Peptide (1-22) via intravenous injection into the tail vein (20 nmol/kg) or subcutaneous injection into the back (50 nmol/kg). CNP is transported across the vascular wall and reaches NPR-B in peripheral tissues. Mouse Convulsion Study: Intracerebroventricular administration of the peptide at 2 nmol is used to assess effects on picrotoxin-kindled convulsions.
ADME/Pharmacokinetics
In conscious sheep, the metabolic clearance rate of CNP is 2.48-3.15 L/min with a half-life of approximately 1.6 minutes after termination of infusion. In rats, following intravenous injection at 20 nmol/kg, the pharmacokinetic parameters are: AUC₀-∞ 320±54 pM·min/mL, T₁/₂ 1.42±0.45 minutes, total clearance 63.9±11.9 mL/min/kg. Following subcutaneous administration at 50 nmol/kg, Cmax is 9.02±3.74 pM/mL, Tmax is 5.0 minutes, AUC₀-∞ is 152±73 pM·min/mL, T₁/₂ is 10.0±5.0 minutes, and bioavailability is 19±9%. The compound has a solubility of 2 mg/mL in DMSO with ultrasonication, and should be stored at -20°C dry and sealed.
Toxicity/Toxicokinetics
According to Safety Data Sheets, C-Type Natriuretic Peptide (CNP) (1-22), human TFA is classified as a non-hazardous substance or mixture with no GHS hazard label elements. Regarding carcinogenicity, it is not listed as hazardous by NTP, IARC, OSHA, or ACGIH. However, toxicity studies indicate that human CNP(1-22) produces mild toxicity at a dose of 2 nM 24 and 48 hours after application, manifested as an increase in convulsion severity. The detailed toxicological effects of this product have not been thoroughly studied. It is for research use only and is not intended for diagnostic, therapeutic, or veterinary use.
References

[1]. ASB20123: A novel C-type natriuretic peptide derivative for treatment of growth failure and dwarfism. PLoS One. 2019 Feb 22;14(2):e0212680.

[2]. Circulating C-type natriuretic peptide is increased in orthotopic cardiac transplant recipients and associated with cardiac allograft vasculopathy. Clin Sci (Lond). 2000 Nov;99(5):467-72.

[3]. ANP(1-28), BNP(1-32) and CNP(1-22) increase the severity of picrotoxin-kindled seizure syndrome in rats. Life Sci. 1993;52(3):PL19-24.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C95H158F3N27O30S3
Molecular Weight
2311.62
Exact Mass
2311.081
CAS #
1966153-17-2
Related CAS #
C-Type Natriuretic Peptide (CNP) (1-22), human;127869-51-6
PubChem CID
168013159
Sequence
H-Gly-Leu-Ser-Lys-Gly-Cys(1)-Phe-Gly-Leu-Lys-Leu-Asp-Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu-Gly-Cys(1)-OH.TFA
glycyl-L-leucyl-L-seryl-L-lysyl-glycyl-L-cysteinyl-L-phenylalanyl-glycyl-L-leucyl-L-lysyl-L-leucyl-L-alpha-aspartyl-L-arginyl-L-isoleucyl-glycyl-L-seryl-L-methionyl-L-seryl-glycyl-L-leucyl-glycyl-L-cysteine (6->22)-disulfide trifluoroacetic acid
SequenceShortening
GLSKGCFGLKLDRIGSMSGLGC
Appearance
White to off-white solid powder
Hydrogen Bond Donor Count
33
Hydrogen Bond Acceptor Count
40
Rotatable Bond Count
44
Heavy Atom Count
158
Complexity
4570
Defined Atom Stereocenter Count
11
SMILES
C(C1C=CC=CC=1)[C@H]1C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@]([H])(C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(NCC(N[C@@H](CSSC[C@@H](C(N1)=O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)CN)C(=O)O)=O)=O)CC(C)C)=O)=O)CO)=O)CCSC)=O)CO)=O)=O)[C@@H](C)CC)=O)CCCNC(N)=N)=O)CC(=O)O)=O)CC(C)C)=O)CCCCN)=O)CC(C)C)=O)=O.C(F)(F)(F)C(=O)O
InChi Key
PKYLOAOOPXCZHF-STACGKDVSA-N
InChi Code
InChI=1S/C93H157N27O28S3.C2HF3O2/c1-12-52(10)76-91(146)104-42-72(127)108-65(44-122)88(143)114-57(26-30-149-11)82(137)118-64(43-121)80(135)103-39-70(125)106-58(31-48(2)3)78(133)101-41-74(129)110-68(92(147)148)47-151-150-46-67(109-73(128)40-100-77(132)54(23-16-18-27-94)111-89(144)66(45-123)119-85(140)59(32-49(4)5)105-69(124)37-96)90(145)116-62(35-53-21-14-13-15-22-53)79(134)102-38-71(126)107-60(33-50(6)7)84(139)112-55(24-17-19-28-95)81(136)115-61(34-51(8)9)86(141)117-63(36-75(130)131)87(142)113-56(83(138)120-76)25-20-29-99-93(97)98;3-2(4,5)1(6)7/h13-15,21-22,48-52,54-68,76,121-123H,12,16-20,23-47,94-96H2,1-11H3,(H,100,132)(H,101,133)(H,102,134)(H,103,135)(H,104,146)(H,105,124)(H,106,125)(H,107,126)(H,108,127)(H,109,128)(H,110,129)(H,111,144)(H,112,139)(H,113,142)(H,114,143)(H,115,136)(H,116,145)(H,117,141)(H,118,137)(H,119,140)(H,120,138)(H,130,131)(H,147,148)(H4,97,98,99);(H,6,7)/t52-,54-,55?,56-,57?,58-,59-,60-,61-,62?,63?,64-,65?,66-,67?,68-,76-;/m0./s1
Chemical Name
(4R,10S,16S,28S,31S,37S,43S)-52-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]acetyl]amino]-40-(4-aminobutyl)-49-benzyl-28-[(2S)-butan-2-yl]-31-(3-carbamimidamidopropyl)-34-(carboxymethyl)-16,22-bis(hydroxymethyl)-10,37,43-tris(2-methylpropyl)-19-(2-methylsulfanylethyl)-6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51-hexadecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35,38,41,44,47,50-hexadecazacyclotripentacontane-4-carboxylic acid;2,2,2-trifluoroacetic acid
Synonyms
C-Type Natriuretic Peptide (CNP) (1-22), human TFA; 1966153-17-2; orb1691348; PD078938; glycyl-L-leucyl-L-seryl-L-lysylglycyl-L-cysteinyl-L-phenylalanylglycyl-L-leucyl-L-lysyl-L-leucyl-L-alpha-aspartyl-L-arginyl-L-isoleucylglycyl-L-seryl-L-methionyl-L-serylglycyl-L-leucylglycyl-L-cysteinecyclic(6-->22)-disulfide,trifluoroacetatesalt
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
H2O: 2 mg/mL (0.87 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.4326 mL 2.1630 mL 4.3260 mL
5 mM 0.0865 mL 0.4326 mL 0.8652 mL
10 mM 0.0433 mL 0.2163 mL 0.4326 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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