Home GPCR & G Protein cAMP inhibitor PACAP 1-27

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PACAP 1-27 cAMP inhibitor

Cat.No.S8414

Pituitary adenylate cyclase activating polypeptide (PACAP 1-27) is a potent PACAP receptor antagonist.
PACAP 1-27 cAMP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 3147.61

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Chemical Information, Storage & Stability

Molecular Weight 3147.61 Formula

C142H224N40O39S

 Storage (From the date of receipt)
CAS No. 127317-03-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC(C)C(C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)O)C(=O)NC(CC(=O)O)C(=O)NC(CO)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCSC)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CC4=CC=C(C=C4)O)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)N)NC(=O)CNC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(CC5=CNC=N5)N

Solubility

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
PACAP receptor [1]
In vitro
PACAP27(100 nM) inhibits all Tat-mediated toxic effects including DNA DSBs, and it prevents the induction of neuronal loss induced by Tat(transactivator of transcription). PACAP27, through CCL5, mitigates the effects of Tat-induced neuronal dysfunction exerting its neuroprotective effect[4]. PACAP-27 (EC50=10nM) stimulates glibenclamide-sensitive and DIDS-insensitive iodide efflux in Calu-3 cells[5].
In vivo
PACAP-27 is potent VIP-like vasodilators of the femoral arterial bed in dogs. In the cardiovascular system, PACAP27 has vasodepressor actions similar to VIP in anesthetized rats. Intra-arterial infusion of PACAP27 induces dose-related increases in peak femoral arterial flow[3].
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24696163/
  • [5] https://pubmed.ncbi.nlm.nih.gov/14744818/

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