PA-915
Based on 1 publication(s) in Google Scholar
PA-915 (PAC1R antagonist 1) is a potent and orally active antagonist of PAC1 receptor. PA-915 inhibits pituitary adenylate cyclase-activating polypeptide (PACAP)-induced CREB phosphorylation. PA-915 can inhibit PACAP- and nerve injury-induced allodynia. PA-915 can be used for the research of neuropathic pain.
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 2305204-24-2
- Formula: C17H17ClN6O2
- Molecular Weight:372.81
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PA-915
MoreAll PACAP Receptor Isoforms
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Biological Activity
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PAC1 Receptor |
PA-915 (Compound 3d) (10 pM-10 nM; 30 min) potently inhibits pituitary
adenylate cyclase-activating polypeptide (PACAP)-induced CREB phosphorylation in PAC1/CHO cells with an IC50 of <10 pM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PAC1 receptor-expressing CHO (PAC1/CHO) cells
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Concentration:10 pM, 100 pM, 1 nM, 10 nM (pre-incubated prior to PACAP stimulation)
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Incubation Time:30 min (pre-incubation prior to 30 min PACAP stimulation)
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Result:Reduced PACAP-induced CREB phosphorylation to 11.9% ± 8.5% of control levels at 1 nM.
Dose-dependently inhibited PACAP-induced CREB phosphorylation, with an IC50 of <10 pM.
PA-915 (100 pmol; i.t.) significantly attenuates established SNL-induced mechanical allodynia in male ddY mice, with peak effects at 2-3 hours post-administration[1].
PA-915 (30 mg/kg; p.o.) significantly reduces established SNL-induced mechanical allodynia in male ddY mice, with peak effects at 3 hours post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, six weeks old at study start)[1]
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Dosage:100 pmol
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Administration:I.t.; single injection
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Result:Significantly blocked the induction of PACAP-induced long-lasting mechanical allodynia, with effects more potent than those of PA-9.
Maintained the 50% paw withdrawal threshold at near-pre-injection levels for at least 7 days post-treatment.
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Animal Model:ddY mice (male, six weeks old at study start)[1]
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Dosage:30 mg/kg
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Administration:P.o.; single administration
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Result:Significantly ameliorated SNL-induced mechanical allodynia in the ipsilateral hind paw.
Reached peak inhibitory effect at 3 hours post-administration and persisted for at least 24 hours.
Caused no effect on paw withdrawal responses in the contralateral paw.
Chemical Information
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CAS No. 2305204-24-2
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Appearance Solid
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Molecular Weight 372.81
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Formula C17H17ClN6O2
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Color White to off-white
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SMILES
O=C(C1CC(N(C1)C2=NNC3=C2C=CC=C3Cl)=O)NCCC4=CNC=N4
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Synonyms
PAC1R antagonist 1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Design of peptide-based PAC1 antagonists combining molecular dynamics simulations and a biologically relevant cell-based assay. [Abstract]2025 May 9:2025.04.16.649181. PMID: 40568092
Solvent & Solubility
DMSO : 33.33 mg/mL (89.40 mM; ultrasonic and warming and heat to 160°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.71 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.71 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6823 mL | 13.4117 mL | 26.8233 mL | 67.0583 mL |
| 5 mM | 0.5365 mL | 2.6823 mL | 5.3647 mL | 13.4117 mL | |
| 10 mM | 0.2682 mL | 1.3412 mL | 2.6823 mL | 6.7058 mL | |
| 15 mM | 0.1788 mL | 0.8941 mL | 1.7882 mL | 4.4706 mL | |
| 20 mM | 0.1341 mL | 0.6706 mL | 1.3412 mL | 3.3529 mL | |
| 25 mM | 0.1073 mL | 0.5365 mL | 1.0729 mL | 2.6823 mL | |
| 30 mM | 0.0894 mL | 0.4471 mL | 0.8941 mL | 2.2353 mL | |
| 40 mM | 0.0671 mL | 0.3353 mL | 0.6706 mL | 1.6765 mL | |
| 50 mM | 0.0536 mL | 0.2682 mL | 0.5365 mL | 1.3412 mL | |
| 60 mM | 0.0447 mL | 0.2235 mL | 0.4471 mL | 1.1176 mL | |
| 80 mM | 0.0335 mL | 0.1676 mL | 0.3353 mL | 0.8382 mL |
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