| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The primary targets of Proinsulin C-peptide are not a single receptor but rather multiple cellular pathways. It has been shown to inhibit high glucose-induced upregulation of PDGF-beta receptor protein expression and the phosphorylation of p42/p44 MAP kinase. It also enhances the deformability of erythrocytes in type 1 diabetes and suppresses the proliferation of rat aortic smooth muscle cells under hyperglycemic conditions. These activities suggest that C-peptide may interact with a specific receptor or signaling complex to exert its physiological effects.
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| ln Vitro |
In vitro, Proinsulin C-peptide (human) has been shown to inhibit high glucose-induced upregulation of PDGF-beta receptor protein expression and the phosphorylation of p42/p44 MAP kinase. This peptide enhances the deformability of erythrocytes in type 1 diabetes, suggesting a role in improving microcirculation. Furthermore, it suppresses the proliferation of rat aortic smooth muscle cells under hyperglycemic conditions, which has potential implications for preventing vascular complications in diabetes. These activities indicate that C-peptide is not merely a byproduct but a bioactive peptide.
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| ln Vivo |
In vivo, Proinsulin C-peptide is an endogenous peptide that plays a role in the regulation of cellular function. Its immunoassay is used to assess pancreatic beta-cell function in diabetic patients. In type 1 diabetes, where insulin and C-peptide are both deficient, its physiological roles become more apparent. It influences a wide variety of physiological processes. Studies suggest that C-peptide replacement may have beneficial effects on diabetic complications, particularly those affecting the vascular system and nerve function, by improving microvascular blood flow and reducing oxidative stress.
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| Enzyme Assay |
Cell-free receptor binding assays for Proinsulin C-peptide are challenging due to the lack of a defined, universally accepted receptor. However, binding studies can be performed using membrane preparations from cells known to respond to C-peptide, such as renal tubular cells or endothelial cells. A typical protocol involves incubating the membranes with a radiolabeled C-peptide (e.g., [125I]-C-peptide) and varying concentrations of unlabeled C-peptide. Bound and free ligand are separated by centrifugation, and the radioactivity is measured. The binding affinity (Kd) can be estimated from saturation binding or competition experiments.
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| Cell Assay |
For in vitro cellular experiments, cells such as renal tubular cells, endothelial cells, or smooth muscle cells are cultured in appropriate media. Cells are treated with Proinsulin C-peptide at various concentrations (typically 1-100 nM) under normal or high-glucose conditions. The effects on signaling pathways are assessed by Western blotting using phospho-specific antibodies (e.g., phospho-p42/p44 MAPK, phospho-PDGF-beta receptor). Cell proliferation is measured using [3H]-thymidine incorporation or MTT assays. Erythrocyte deformability can be assessed using a filtration technique.
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| Animal Protocol |
In vivo animal experiments with Proinsulin C-peptide are typically conducted in rodent models of type 1 diabetes, such as streptozotocin (STZ)-induced diabetic rats or mice. A common protocol involves administering human C-peptide via subcutaneous or intraperitoneal infusion using mini-osmotic pumps at doses that mimic physiological levels (e.g., 50-100 pmol/kg/min). The compound's effects on diabetic complications are assessed by measuring nerve conduction velocity, vascular function, and renal parameters. Blood glucose is monitored to ensure the effects are independent of insulin.
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| ADME/Pharmacokinetics |
Proinsulin C-peptide human is a peptide with a molecular weight of 3020.26 g/mol and a molecular formula of C129H211N35O48. As a peptide, it is administered parenterally, as it would be degraded in the gastrointestinal tract if given orally. Its half-life in circulation is relatively short, typically on the order of 20-30 minutes, necessitating continuous infusion or frequent injections in experimental settings. It is stable as a powder at -20degC for up to 3 years and soluble in aqueous buffers.
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| Toxicity/Toxicokinetics |
The toxicity profile of Proinsulin C-peptide is favorable, as it is an endogenous peptide. No significant toxicity has been reported in preclinical or clinical studies at doses that achieve physiological or slightly supraphysiological levels. High doses are generally well-tolerated. However, as with any peptide, there is a potential for immunogenicity, although this has not been a major issue in studies to date. It is for research use only and not for human therapeutic use.
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| Additional Infomation |
C-peptide is being investigated in the clinical trial NCT00278980 (Effects of C-peptide on diabetic peripheral neuropathy). C-peptide is an intermediate fragment of proinsulin, located between the N-terminal B chain and the C-terminal A chain. It is a pancreatic peptide composed of approximately 31 amino acid residues, the exact length depending on the species. Proinsulin, upon proteolysis, releases an equimolar amount of insulin and C-peptide. C-peptide immunoassay has been used to assess pancreatic β-cell function in diabetic patients with circulating insulin antibodies or those receiving exogenous insulin therapy. C-peptide has a half-life of 30 minutes, almost eight times that of insulin.
Proinsulin C-peptide human is a 31-amino acid peptide that links the A and B chains of proinsulin, facilitating its correct folding. It is a bioactive molecule that inhibits high glucose-induced PDGF-beta receptor expression and MAP kinase phosphorylation. It also enhances erythrocyte deformability and suppresses smooth muscle cell proliferation. Its immunoassay is a key measure of beta-cell function in diabetes. It is a valuable research tool for studying diabetes and its complications. |
| Molecular Formula |
C129H211N35O48
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|---|---|
| Molecular Weight |
3020.26133999999
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| Exact Mass |
3018.51
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| CAS # |
33017-11-7
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| PubChem CID |
16157840
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| Appearance |
White to off-white solid powder
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| LogP |
-12.6
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| Hydrogen Bond Donor Count |
41
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| Hydrogen Bond Acceptor Count |
49
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| Rotatable Bond Count |
101
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| Heavy Atom Count |
212
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| Complexity |
7190
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| Defined Atom Stereocenter Count |
24
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| SMILES |
OCCC(NCC(N[C@@H](CCC(N)=O)C(N1[C@H](C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(NCC(N[C@@H](CO)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(N)=O)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)=O)=O)=O
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| InChi Key |
VOUAQYXWVJDEQY-QENPJCQMSA-N
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| InChi Code |
InChI=1S/C129H211N35O48/c1-58(2)42-77(155-113(195)74(31-39-102(184)185)151-127(209)105(65(15)16)162-114(196)71(25-32-88(131)167)145-95(174)54-141-126(208)104(64(13)14)161-115(197)72(26-33-89(132)168)150-118(200)80(45-61(7)8)156-121(203)83(48-103(186)187)159-112(194)73(30-38-101(182)183)148-107(189)67(18)143-109(191)69(130)24-36-99(178)179)111(193)138-50-93(172)135-49-92(171)136-55-98(177)163-40-20-22-86(163)124(206)140-51-94(173)142-66(17)106(188)137-52-96(175)146-84(56-165)122(204)157-81(46-62(9)10)119(201)152-75(27-34-90(133)169)128(210)164-41-21-23-87(164)125(207)160-78(43-59(3)4)116(198)144-68(19)108(190)154-79(44-60(5)6)117(199)149-70(29-37-100(180)181)110(192)139-53-97(176)147-85(57-166)123(205)158-82(47-63(11)12)120(202)153-76(129(211)212)28-35-91(134)170/h58-87,104-105,165-166H,20-57,130H2,1-19H3,(H2,131,167)(H2,132,168)(H2,133,169)(H2,134,170)(H,135,172)(H,136,171)(H,137,188)(H,138,193)(H,139,192)(H,140,206)(H,141,208)(H,142,173)(H,143,191)(H,144,198)(H,145,174)(H,146,175)(H,147,176)(H,148,189)(H,149,199)(H,150,200)(H,151,209)(H,152,201)(H,153,202)(H,154,190)(H,155,195)(H,156,203)(H,157,204)(H,158,205)(H,159,194)(H,160,207)(H,161,197)(H,162,196)(H,178,179)(H,180,181)(H,182,183)(H,184,185)(H,186,187)(H,211,212)/t66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,104-,105-/m0/s1
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| Chemical Name |
(4S)-4-amino-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[2-[[2-[(2S)-2-[[2-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(1S)-4-amino-1-carboxy-4-oxobutyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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) |
DMSO : ≥ 60 mg/mL (~19.87 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 | 0.3311 mL | 1.6555 mL | 3.3110 mL | |
| 5 mM | 0.0662 mL | 0.3311 mL | 0.6622 mL | |
| 10 mM | 0.0331 mL | 0.1655 mL | 0.3311 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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