Home GPCR & G Protein cAMP inhibitor PACAP 6-38 acetate

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PACAP 6-38 acetate cAMP inhibitor

Cat.No.S8416

PACAP 6-38 acetate is a PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM. It also acts as a functional CARTp antagonist in vivo.
PACAP 6-38 acetate cAMP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 4083.74

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Quality Control

Batch: Purity: 99.63%
99.63

Solubility

In vitro
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Water : 100 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 4083.74 Formula

C182H300N56O45S

 Storage (From the date of receipt)
CAS No. 143748-18-9(free base) Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CSCCC(NC(=O)C(CCC(N)=O)NC(=O)C(CCCCN)NC(=O)C(CCCNC(N)=N)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(CCCNC(N)=N)NC(=O)C(CO)NC(=O)C(CC2=CC=C(O)C=C2)NC(=O)C(CO)NC(=O)C(CC(O)=O)NC(=O)C(NC(=O)C(N)CC3=CC=CC=C3)C(C)O)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CC4=CC=C(O)C=C4)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NC(CC(C)C)C(=O)NCC(=O)NC(CCCCN)C(=O)NC(CCCNC(N)=N)C(=O)NC(CC5=CC=C(O)C=C5)C(=O)NC(CCCCN)C(=O)NC(CCC(N)=O)C(=O)NC(CCCNC(N)=N)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(N)=O)C(=O)NC(CCCCN)C(N)=O

Mechanism of Action

Targets/IC50/Ki
CARTp
PACAP receptor
2 nM
In vitro

PACAP 6-38 blocks the CARTp-induced phosphorylation of ERK in differentiated cells.
In vivo

Intravesical administration of the PAC1 receptor antagonist, PACAP(6-38) (300 nM), significantly (p ≤ 0.01) increases intercontraction interval (2.0-fold) and void volume (2.5-fold) in NGF-OE mice. PACAP(6-38) has no effects on bladder function in WT mice. Intravesical administration of PACAP(6–38) (300 nM) significantly (p ≤ 0.01) reduces pelvic sensitivity in NGF-OE mice but is without effect in WT mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/27146136/

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