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PACAP (1-38), human, ovine, rat TFA

Alias: Pituitary Adenylate Cyclase Activating Polypeptide 38 TFA
Cat No.:V142108 Purity: ≥98%
PACAP (1-38), human, ovine, rat TFA is a PAC1 receptor agonist.
PACAP (1-38), human, ovine, rat TFA
PACAP (1-38), human, ovine, rat TFA Chemical Structure Product category: Calcium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes
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Product Description
PACAP (1-38), human, ovine, and rat TFAs, are PAC1 receptor agonists. PACAP (1-38) (human, sheep, and rat) binds to PACAP type I receptors, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively, with IC50 values of 4 nM, 2 nM, and 1 nM. PACAP (1-38) (human, sheep, and rat) increases α-secretase activity. PACAP (1-38) (human, sheep, and rat) increases cytoplasmic Ca2+ concentration, promotes cell proliferation, and increases the phosphorylation levels of extracellular signal-regulated kinase (ERK) and epidermal growth factor receptor (EGFR). PACAP (1-38) (human, sheep, and rat) has a potent, efficient, and sustained stimulatory effect on the production of NPY and catecholamines in sympathetic neurons. PACAP (1-38), human, sheep, and rat TFAs can be used in neurotrophic and neuroprotective studies.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
PACAP (1-38), human, sheep, and rat trifluoroacetate (TFA), is a fragment of the pituitary adenylate cyclase activating peptide [1]. PACAP (1-38), human, sheep, and rat trifluoroacetate has a high affinity for PACAP-specific receptor (PAC1) on the membranes of various tissues, including the endocrine pancreas [2]. In vitro experiments have shown that PACAP (1-38), human, sheep, and rat trifluoroacetate can relax histamine and acetylcholine-precontracted tracheal smooth muscle in guinea pigs and rabbits. PACAP (1-38) can also increase the level of cyclic adenosine monophosphate (cAMP) in tracheal smooth muscle, which provides a possible mechanism for the relaxing effect of PACAP (1-38) [3]. PACAP (1-38), human, sheep, and rat TFA (100 nM; 2 min; NCI-H838 cells) can induce EGFR, HER2, and ERK tyrosine phosphorylation [5]. PACAP (1-38), human, sheep, and rat TFA (100 nM; 30 min; NCI-H838 cells) can induce EGFR tyrosine phosphorylation and produce ROS, increasing ROS levels by 51% [5]. PACAP (1-38), human, sheep, and rat TFA (10 nM; 48 h) can stimulate the growth of NCI-H838 cells [5]. PACAP (1-38), human, sheep, and rat TFA (300 nM; 4 h) can stimulate the production of APPsα in nerve cells [6]. PACAP (1-38), human, sheep, and rat trifluoroacetic acid (TFA) (0.01-10 nM; HEK 293 cells) stimulates the expression of endogenous PAC1 receptors in nerve cells through cAMP accumulation and increased cytoplasmic free calcium, and induces an increase in intracellular Ca2+ concentration in a dose-dependent manner, with an EC50 value of 0.81 nM [6]. PACAP (1-38), human, sheep, and rat trifluoroacetic acid (TFA) (0.01 nM; 48 hours) can strongly stimulate SCG neuron cultures to secrete NPY [7]. PACAP (1-38), human, sheep, and rat trifluoroacetic acid (TFA) (100 nM; 14 days) can continuously stimulate sympathetic neurons to secrete NPY and catecholamines [7].
ln Vivo
In sham-operated animals, the use of PACAP (1-38), human, sheep and mouse TFA alone did not cause any changes in the retinal layer. Dissolving PACAP (1-38), human, sheep and mouse TFA in benzalkonium chloride-containing eye drops significantly protected the retina of bilateral common carotid artery occlusion (BCCAO) injury; the retinal structure treated with PACAP (1-38) eye drops was preserved compared with the control retina[4].
Cell Assay
Cell viability assay [1]
Cell Types: NCI-H838 cells
Tested Concentrations: 10 nM
Incubation Duration: 48 hours
Experimental Results: The number of NCI-H838 cells increased by 72%.
Western Blot Analysis [1]
Cell Types: NCI-H838 cells
Tested Concentrations: 100 nM
Incubation Duration: 2 minutes
Experimental Results: Tyrosine phosphorylation of EGFR, HER2 and ERK increased by 377%, 299% and 216%, respectively.
References

[1]. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11.

[2]. Yamaguchi N. Pituitary adenylate cyclase activating polypeptide enhances glucose-evoked insulin secretion in the canine pancreas in vivo. JOP. 2001 Sep;2(5):306-16.

[3]. Inhibition of bronchoconstriction by pituitary adenylate cyclase activating polypeptide (PACAP 1-27) in guinea-pigs in vivo. Br J Pharmacol. 1995 Jul;115(6):913-6.

[4]. Passage through the Ocular Barriers and Beneficial Effects in Retinal Ischemia of Topical Application of PACAP (1-38) in Rodents. Int J Mol Sci. 2017 Mar 21;18(3). pii: E675.

[5]. PAC1 regulates receptor tyrosine kinase transactivation in a reactive oxygen species-dependent manner. Peptides. 2019 Oct;120:170017.

[6]. The neuropeptide PACAP promotes the alpha-secretase pathway for processing the Alzheimer amyloid precursor protein. FASEB J. 2006 Mar;20(3):512-4.

[7]. Pituitary adenylate cyclase-activating polypeptides, PACAP-38 and PACAP-27, regulation of sympathetic neuron catecholamine, and neuropeptide Y expression through activation of type I PACAP/VIP receptor isoforms. Ann N Y Acad Sci. 1996 Dec 26;805:204-16; discussion 217-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C203H331N63O53S.C2HF3O2
Molecular Weight
4534.26 (free base)
Sequence
His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys-NH2HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK-NH2
SequenceShortening
HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK-NH2
Appearance
Typically exists as solids at room temperature
Synonyms
Pituitary Adenylate Cyclase Activating Polypeptide 38 TFA
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

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
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.)
Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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