PACAP 1-38

Catalog No.S8415 Batch:S841501

Technical Data

Formula	C₂₀₃H₃₃₁N₆₃O₅₃S
Molecular Weight	4534.26	CAS No.	137061-48-4
Solubility (25°C)*	In vitro	Water	100 mg/mL (22.05 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

PACAP 1-38 (Pituitary Adenylate Cyclase Activating Polypeptide 38) is a highly potent PACAP receptor agonist (Kd = 100 pM). It stimulates adenylate cyclase and phagocytosis.

Targets

PAC1 ^[3]	PAC1s ^[3]	PAC1vs ^[3]
1.1 nM(Ki)	1.7 nM(Ki)	121 nM(Ki)

In vitro

PACAP 1-38 has potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production^[1]. It is a pleiotropic neuropeptide, exhibiting a variety of biologic actions, including activities as a neurotransmitter, neuromodulator, neurotrophic factor, as well as an immunomodulator, in immune cells through its effect on MAPK signaling and modulation of activation of NFκB. PACAP 1-38 dramatically prevents injury of cultured renal proximal tubule cells caused by myeloma light chains through suppression of proinflammatory cytokines production, by inhibiting p38 MAPK and translocation of NFκB via both PAC1 and VPAC1 receptors. PACAP38 inhibits myeloma cell growth directly and may also indirectly by suppressing production of the growth factor, IL-6, from bone marrow stromal cells, that is stimulated by adhesion of myeloma cells. PACAP38 suppressed release of both IL-6 and TNFα dose dependently^[2].

In vivo

PACAP38 is capable of inhibiting light chain-induced cytokine expression with a great potency and prevented the resulting cell damage in vivo. However, PACAP is also considered as an autoregulatory factor for certain tumors, stimulating their growth in an autocrine fashion^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines human renal proximal tubule cell line Concentrations 0.0001-100 nM Incubation Time 3 days Method Human renal proximal tubule cells plated onto 6-well tissue culture plates are grown at 37°C in DRM-23E medium supplemented with 0.5% (vol/vol) FBS in an incubator for 24 hours. After prewashing with serum-free medium, the cells are incubated with κ-LC (1.5 mg/ml, ∼ 50 μM) for 3 days in the presence and absence of various concentrations of PACAP38 or dexamethasone as well as kinase and transcription factor inhibitors. Cell viability is determined by trypan blue exclusion assays; in all experiments, at least 85% of cells remain viable. After exposure to test substances, culture supernatants are harvested and stored at –70°C for cytokine assays. After the medium is removed, the cells are washed with ice-cold PBS, and proteins are extracted by lysing cells with Sigma Mammalian Cell Lysis Reagents. Lysates are scraped and passed through a 21-gauge needle to shear DNA, and centrifuged at 12 000g for 10 minutes at 4°C. Finally, supernatants are harvested and used for kinase studies.
Animal Study:^{^[2]}	Animal Models Male Sprague-Dawley rats Dosages 2 nmol/10 mL Administration i.v.

Cell Assay:^{^[2]}

Cell lines
human renal proximal tubule cell line
Concentrations
0.0001-100 nM
Incubation Time
3 days
Method
Human renal proximal tubule cells plated onto 6-well tissue culture plates are grown at 37°C in DRM-23E medium supplemented with 0.5% (vol/vol) FBS in an incubator for 24 hours. After prewashing with serum-free medium, the cells are incubated with κ-LC (1.5 mg/ml, ∼ 50 μM) for 3 days in the presence and absence of various concentrations of PACAP38 or dexamethasone as well as kinase and transcription factor inhibitors. Cell viability is determined by trypan blue exclusion assays; in all experiments, at least 85% of cells remain viable. After exposure to test substances, culture supernatants are harvested and stored at –70°C for cytokine assays. After the medium is removed, the cells are washed with ice-cold PBS, and proteins are extracted by lysing cells with Sigma Mammalian Cell Lysis Reagents. Lysates are scraped and passed through a 21-gauge needle to shear DNA, and centrifuged at 12 000g for 10 minutes at 4°C. Finally, supernatants are harvested and used for kinase studies.

Animal Study:^{^[2]}

Animal Models
Male Sprague-Dawley rats
Dosages
2 nmol/10 mL
Administration
i.v.

References

Selleck's PACAP 1-38 has been cited by 4 publications

Intravitreal Injection of PACAP Attenuates Acute Ocular Hypertension-Induced Retinal Injury Via Anti-Apoptosis and Anti-Inflammation in Mice [ Invest Ophthalmol Vis Sci, 2022, 63(3):18]	PubMed: 35293951
PAC1 Receptor Mediates Electroacupuncture-Induced Neuro and Immune Protection During Cisplatin Chemotherapy [ Front Immunol, 2021, 12:714244]	PubMed: 34552585
PACAP causes PAC1/VPAC2 receptor mediated hypertension and sympathoexcitation in normal and hypertensive rats [ Am J Physiol Heart Circ Physiol, 2012, 303(7):H910-7]	PubMed: 22886412
PACAP causes PAC1/VPAC2receptor mediated hypertension and sympathoexcitation in normal and hypertensive rats [ American Journal of Physiology-Heart and Circulatory Physiology, 2012, Vol. 303, No. 7]	PubMed: None

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SHIPPING AND STORAGE
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