2. GPCR/G Protein
  3. Adenosine Receptor
  4. PSB36

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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PSB36

PSB36 Chemical Structure

CAS No. : 524944-72-7

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Based on 1 publication(s) in Google Scholar

PSB36 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PSB36

View All Adenosine Receptor Isoform Specific Products:

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

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.

PSB36 Related Antibodies
In Vivo

PSB36 (30-100 mg/kg; i.p.) produces no analgesic effect in the mouse hot plate model of acute thermal pain[1].
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.

Animal Model: NMRI (male, 32-40 g)[2]
Dosage: 10 mg/kg (edema); 30 mg/kg (edema); 100 mg/kg (early-phase nociceptive behavior); 1% suspension (local co-injection)
Administration: i.p. (30 minutes before formalin injection); local co-injection with formalin
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.
Animal Model: NMRI (male, 32-40 g)[2]
Dosage: 30 mg/kg (edema at 80 minutes); 100 mg/kg (edema at 30, 80, 120 minutes)
Administration: i.p. (30 minutes before carrageenan injection)
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.
Molecular Weight

386.49

Formula

C21H30N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCCC)N(CCCO)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5874 mL 12.9369 mL 25.8739 mL
5 mM 0.5175 mL 2.5874 mL 5.1748 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.94%

SDS (254 KB)

COA (252 KB) HNMR (143 KB) RP-HPLC (169 KB) LCMS (234 KB)

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 2.5874 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
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PSB36 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PSB36524944-72-7PSB 36PSB-36Adenosine ReceptorP1 receptoradenosine receptorhuman atrial APD90mouseinflammatory painedemainflammatory hyperalgesiaatrial ERPatrial fibrillationInhibitorinhibitorinhibit

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