PSB36
Based on 1 publication(s) in Google Scholar
PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation.
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- Pureza : 99.13%
- No. CAS: 524944-72-7
- Fòrmula: C21H30N4O3
- Peso molecular:386.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PSB36
MoreVer todos los productos específicos de isoformas Adenosine Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
rA1 0.12 nM (Ki) |
hA2B 187 nM (Ki) |
rA2A 552 nM (Ki) |
hA3 2300 nM (Ki) |
rA3 6500 nM (Ki) |
In Vitro
PSB36 (1 μM; 10 min) significantly prolongs APD90 in intact trabeculae isolated from human right atrial appendages from patients in sinus rhythm[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Systemic administration of PSB36 (10-100 mg/kg; i.p.; single dose) significantly reduces formalin-induced hind paw edema and early phase inflammatory pain, whereas no such effect is observed with local administration[2].
Systemic administration of PSB36 (10-100 mg/kg; i.p.; single dose) significantly reduces carrageenan-induced hind paw edema[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI (male, 32-40 g)[2]
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Dosage:10 mg/kg (edema); 30 mg/kg (edema); 100 mg/kg (early-phase nociceptive behavior); 1% suspension (local co-injection)
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Administration:i.p. (30 minutes before formalin injection); local co-injection with formalin
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Result:Reduced formalin-induced edema by 32.5%.
Reduced formalin-induced edema by 36.3%.
Produced a significant 31.8% reduction in nociceptive behavior in the early irritant phase.
Showed no effect on edema, early phase pain, or late phase pain when administered locally.
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Animal Model:NMRI (male, 32-40 g)[2]
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Dosage:30 mg/kg (edema at 80 minutes); 100 mg/kg (edema at 30, 80, 120 minutes)
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Administration:i.p. (30 minutes before carrageenan injection)
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Result:Significantly reduced carrageenan-induced edema at 80 minutes post-carrageenan.
Significantly reduced carrageenan-induced edema at 30, 80, and 120 minutes post-carrageenan.
Showed no significant reduction in carrageenan-induced hyperalgesia at any tested dose.
Chemical Information
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No. CAS 524944-72-7
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Appearance Solid
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Peso molecular 386.49
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Fòrmula C21H30N4O3
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Color White to off-white
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SMILES
O=C(N1CCCC)N(CCCO)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Nature
2026 Jan;649(8096):423-431. PMID: 41193806
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (258.74 mM; Need ultrasonic; 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)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
In Vivo Dissolution Calculator
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.
Protocolo
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Abo-Salem OM, et al. Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004;308(1):358-366. [Content Brief]
[2]. Bilkei-Gorzo A, et al. Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia. Naunyn Schmiedebergs Arch Pharmacol. 2008;377(1):65-76. [Content Brief]
[3]. Soattin L, et al. Inhibition of Adenosine Pathway Alters Atrial Electrophysiology and Prevents Atrial Fibrillation. Front Physiol. 2020;11:493. Published 2020 Jun 12. [Content Brief]
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 | 2.5874 mL | 12.9369 mL | 25.8739 mL | 64.6847 mL |
| 5 mM | 0.5175 mL | 2.5874 mL | 5.1748 mL | 12.9369 mL | |
| 10 mM | 0.2587 mL | 1.2937 mL | 2.5874 mL | 6.4685 mL | |
| 15 mM | 0.1725 mL | 0.8625 mL | 1.7249 mL | 4.3123 mL | |
| 20 mM | 0.1294 mL | 0.6468 mL | 1.2937 mL | 3.2342 mL | |
| 25 mM | 0.1035 mL | 0.5175 mL | 1.0350 mL | 2.5874 mL | |
| 30 mM | 0.0862 mL | 0.4312 mL | 0.8625 mL | 2.1562 mL | |
| 40 mM | 0.0647 mL | 0.3234 mL | 0.6468 mL | 1.6171 mL | |
| 50 mM | 0.0517 mL | 0.2587 mL | 0.5175 mL | 1.2937 mL | |
| 60 mM | 0.0431 mL | 0.2156 mL | 0.4312 mL | 1.0781 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3234 mL | 0.8086 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2587 mL | 0.6468 mL |
PSB36 Related Classifications
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