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PACAP (1-27), human, ovine, rat 127317-03-7

PACAP (1-27), human, ovine, rat 127317-03-7

CAS No.: 127317-03-7

PACAP (1-27), human, ovine, rat (PACAP 1-27) is the N-terminal fragment of PACAP-38 and is a potent PACAP receptor block
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

PACAP (1-27), human, ovine, rat (PACAP 1-27) is the N-terminal fragment of PACAP-38 and is a potent PACAP receptor blocker (antagonist) against rat PAC1, rat VPAC1 and human VPAC2 The IC50s are 3 nM, 2 nM and 5 nM respectively.

Physicochemical Properties


Molecular Formula C142H224N40O39S
Molecular Weight 3147.60755999999
Exact Mass 3145.649
CAS # 127317-03-7
Related CAS # PACAP (1-27), human, ovine, rat TFA
Appearance White to off-white solid powder
Density 1.5±0.1 g/cm3
Index of Refraction 1.657
LogP -3.65
SMILES

0

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)

Biological Activity


ln Vitro Radioligand receptor binding assays using I-monoiodinated PACAP (1-27), human, sheep, rat confirmed the presence of PAC receptors on AR4-2J cells because PACAP (1-27), human, sheep , rat, and PACAP(1–38) equivalently displace radioligand binding with a Kd of 1-2 nM, whereas vasoactive intestinal peptide (VIP) is 1000-fold less potent. PACAP (1-27), humans, sheep, and rats demonstrate significant and increased sensitivity to VIP amino acid changes. PACAP (1-27), human, sheep, rat, has the efficacy and binding affinity to induce the production of IP3 and cAMP in AR4-2J cells [2].
ln Vivo Anesthetized and ventilated guinea pigs were used to study the inhibitory effect of pituitary adenylate cyclase-activating polypeptide (PACAP (1-27), human, sheep, rat) on the increase in total lung resistance (RL) produced by allergens or histamine. By intravenous infusion (0.045-4.5 nmol/kg/min), PACAP (1-27), human, sheep, and rat dose-dependently inhibits the rise in RL caused by inhaled ovalbumin and histamine. When administered at the maximum dosage, PACAP (1–27), human, sheep, and rat all totally stopped the ovalbumin and histamine-induced rise in RL. The β2-adrenoceptor agonist albuterol (0.045-4.5 nmol/kg/min), PACAP (1-27), human, sheep, and rat infusions all blocked increases in RL in a similar way [3]. However, albuterol increased heart rate more than PACAP (1-27), human, sheep, and rat infusions.
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]. Structural motifs of pituitary adenylate cyclase-activating polypeptide (PACAP) defining PAC1-receptor selectivity. Regul Pept. 1999 Feb 5;79(2-3):83-92.

[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.


Solubility Data


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
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 : 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).
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 : PEG300:Tween 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).
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 0.3177 mL 1.5885 mL 3.1770 mL
5 mM 0.0635 mL 0.3177 mL 0.6354 mL
10 mM 0.0318 mL 0.1589 mL 0.3177 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.