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| Targets |
PACAP-38 (31-38) targets the PAC1 receptor (pituitary adenylate cyclase-activating polypeptide type 1 receptor), a G protein-coupled receptor that is activated by PACAP-38. The PAC1 receptor is widely expressed in the nervous system and plays critical roles in neurotransmission, neuroprotection, and neurodevelopment. By activating the PAC1 receptor, PACAP-38 (31-38) increases alpha-secretase activity, elevates cytosolic Ca2+, and increases proliferation and phosphorylation of ERK and EGFR. The peptide has potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38) is used in neurotrophic and neuroprotective research.
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| ln Vitro |
The human, mouse, dependent PACAP-38 (31-38) causes EGFR, HER2, and ERK tyrosine phosphorylation at 100 nM over a 2-minute period in NCI-H838 cells [1]. Human, mouse, and urine (100 nM; 30 minutes; NCI-H838 cells) treated with PACAP-38 (31-38) causes EGFR tyrosine phosphorylation, generates reactive oxygen species, and raises ROS levels by 51% [1]. NCI-H838 cells are stimulated to grow by PACAP-38 (31-38) PACAP-38 (31-38), human, mouse, and rat (300 nM; 48 hours) [1]. Through cAMP accumulation and an increase in solute free calcium, PACAP-38 (31-38), a human, mouse, toxin (0.01-10 nM; HEK 293 cells), stimulates neuronal expression endogenously. With an EC50 value of 0.81 nM, it inhibits PAC1 entry and causes a dose-dependent increase in intracellular Ca2+ concentration [2]. In SCG neuronal cultures, PACAP-38 (31-38), human, mouse, nozzle (0.01 nM; 48 h) efficiently rescues NPY [3]. PACAP-38 (31-38), Human, Mouse, Accountable (100 nM; 14 d) Generates NPY and catecholamine neurons that are sustainedly rescued [3
PACAP-38 (31-38) demonstrates potent in vitro activity as a PAC1 receptor activator. The peptide increases alpha-secretase activity, elevates cytosolic Ca2+, and increases proliferation and phosphorylation of ERK and EGFR. PACAP-38 (31-38) has potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. Its activity is concentration-dependent, with effects observed at appropriate concentrations. The peptide is used in neurotrophic and neuroprotective research. PACAP-38 (31-38) serves as a crucial tool for investigating peptide-receptor binding dynamics and neuropeptide functions. |
| ln Vivo |
In vivo, PACAP-38 (31-38) has been studied for its neurotrophic and neuroprotective effects. As a PAC1 receptor activator, the peptide modulates neurotransmission and provides neuroprotection across various species. PACAP-38 (31-38) has potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. The peptide may be utilized in neurotrophic and neuroprotective research. Its ability to activate PAC1 receptors and modulate neuronal function makes it a valuable tool for studying neuropeptide signaling.
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| Enzyme Assay |
In vitro receptor binding assays for PACAP-38 (31-38) involve measuring binding affinity to the PAC1 receptor. Membranes from cells expressing the PAC1 receptor are incubated with a radiolabeled PACAP ligand and varying concentrations of the test peptide. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. Functional assays can measure receptor activation by assessing cAMP accumulation, calcium mobilization, or ERK phosphorylation. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (full-length PACAP-38) and vehicle controls.
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: NCI-H838 Cell Tested Concentrations: 10 nM Incubation Duration: 48 hrs (hours) Experimental Results: NCI-H838 cell number increased by 72%. Western Blot Analysis[1] Cell Types: 100 nM Tested Concentrations: 100 nM Incubation Duration: 2 minutes Experimental Results: Tyrosine phosphorylation of EGFR, HER2 and ERK increased by 377%, 299% and 216% respectively. In vitro cellular assays for PACAP-38 (31-38) are performed using neuronal cell lines or primary neurons expressing the PAC1 receptor. Cells are treated with varying concentrations of the peptide. Receptor activation is measured by assessing cAMP accumulation using ELISA or HTRF assays. Calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 or Fura-2. ERK and EGFR phosphorylation is assessed by Western blot using phospho-specific antibodies. Cell proliferation is measured using [3H]-thymidine incorporation or CellTiter-Glo assays. alpha-secretase activity can be measured using fluorogenic substrates. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. EC50 values are calculated from dose-response curves. |
| Animal Protocol |
In vivo animal studies for PACAP-38 (31-38) are conducted using rodent models to study neurotrophic and neuroprotective effects. The peptide is administered via intracerebroventricular injection, intravenous injection, or other routes. Neurotransmitter levels (NPY, catecholamines) are measured in tissues by ELISA or HPLC. Behavioral tests are used to assess cognitive function and neuroprotection. Pharmacokinetic studies assess peptide concentrations in plasma and brain tissue. Animals are monitored for clinical signs and body weight. The peptide's effects on neuroprotection and neurotransmission are assessed compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PACAP-38 (31-38) are characteristic of a peptide. The peptide has a molecular formula of C47H83N17O11 and a molecular weight of 1062.27 g/mol. As a peptide, PACAP-38 (31-38) is susceptible to proteolytic degradation and has a relatively short half-life in circulation. The peptide is typically administered by injection due to poor oral bioavailability. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in preclinical studies. The peptide's pharmacokinetic profile supports its use as a research tool.
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| Toxicity/Toxicokinetics |
PACAP-38 (31-38) is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a neuropeptide fragment, the compound is generally well-tolerated at research-use concentrations. Standard in vitro cytotoxicity assays in neuronal cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been extensively reported. The peptide is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
PACAP-38 (31-38), human, mouse, rat is a synthetic peptide fragment corresponding to amino acid residues 31-38 of PACAP-38. It is a PAC1 receptor activator that increases alpha-secretase activity. PACAP-38 (31-38) elevates cytosolic Ca2+ and increases ERK and EGFR phosphorylation and proliferation. The peptide has a molecular formula of C47H83N17O11 and a molecular weight of 1062.27 g/mol. PACAP-38 (31-38) is used in neurotrophic and neuroprotective research. The compound has not entered clinical trials and is available for research purposes only.
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| Molecular Formula |
C47H83N17O11
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| Molecular Weight |
1062.26922
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| Exact Mass |
1061.65
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| CAS # |
138764-85-9
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| Related CAS # |
PACAP-38 (31-38), human, mouse, rat TFA
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| PubChem CID |
139270272
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| Appearance |
White to off-white solid powder
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| LogP |
3.417
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
39
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| Heavy Atom Count |
75
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| Complexity |
1880
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C(C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCC(=O)N)NC(=O)C(CCCCN)NC(=O)C(CC1=CC=C(C=C1)O)N
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| InChi Key |
YJQRDMBVNVOBLN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C47H83N17O11/c1-26(2)38(46(75)62-32(12-5-8-22-50)42(71)63-35(25-37(53)67)45(74)58-30(39(54)68)10-3-6-20-48)64-44(73)33(13-9-23-57-47(55)56)60-43(72)34(18-19-36(52)66)61-41(70)31(11-4-7-21-49)59-40(69)29(51)24-27-14-16-28(65)17-15-27/h14-17,26,29-35,38,65H,3-13,18-25,48-51H2,1-2H3,(H2,52,66)(H2,53,67)(H2,54,68)(H,58,74)(H,59,69)(H,60,72)(H,61,70)(H,62,75)(H,63,71)(H,64,73)(H4,55,56,57)
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| Chemical Name |
N-[1-[[1-[[6-amino-1-[[4-amino-1-[(1,6-diamino-1-oxohexan-2-yl)amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[6-amino-2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]pentanediamide
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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) |
H2O : ~100 mg/mL (~94.14 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 | 0.9414 mL | 4.7069 mL | 9.4138 mL | |
| 5 mM | 0.1883 mL | 0.9414 mL | 1.8828 mL | |
| 10 mM | 0.0941 mL | 0.4707 mL | 0.9414 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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