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

Derenofylline  (Synonyms: SLV 320)

Cat. No.: HY-14858 Purity: 99.87%
COA Handling Instructions

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Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.

For research use only. We do not sell to patients.

Derenofylline Chemical Structure

Derenofylline Chemical Structure

CAS No. : 251945-92-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 97 In-stock
Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Solid
1 mg USD 35 In-stock
5 mg USD 88 In-stock
10 mg USD 143 In-stock
25 mg USD 308 In-stock
50 mg USD 550 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Derenofylline Related Antibodies

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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

Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats[1].

IC50 & Target[1]

A1R

1 nM (Ki)

Adenosine A3 receptor

200 nM (Ki)

A2AR

398 nM (Ki)

In Vitro

Derenofylline (100 μM, 72 h) inhibits TGF-β1-induced myofibroblast transformation without affecting the cell viability[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Derenofylline Related Antibodies
In Vivo

Derenofylline (0.3-10 mg/kg, oral administration) suppresses adenosine-induced bradycardia in rats[1].
Derenofylline (10 mg/kg/d, oral administration, 12 weeks) reduces myocardial fibrosis in 5/6 nephrectomy rats without affecting blood pressure[1].
Derenofylline (0.1-5mg/kg, intravenous injection) causes no major haemodynamic effects (heart rate and blood pressure)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5/6 nephrectomy rats[1]
Dosage: 10 mg/kg/d
Administration: Oral administration, mixed with food for 12 weeks
Result: Attenuated urinary albuminuria by about 50%.
Suppressed the increase in CK levels, ALT and AST plasma levels in nephrectomized animals.
Clinical Trial
Molecular Weight

308.38

Formula

C18H20N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1CC[C@H](NC2=C3C(NC=C3)=NC(C4=CC=CC=C4)=N2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (324.28 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 3.2428 mL 16.2138 mL 32.4275 mL
5 mM 0.6486 mL 3.2428 mL 6.4855 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6.25 mg/mL (20.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 6.25 mg/mL (20.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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:

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: 99.87%

COA (255 KB) LCMS (264 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2428 mL 16.2138 mL 32.4275 mL 81.0688 mL
5 mM 0.6486 mL 3.2428 mL 6.4855 mL 16.2138 mL
10 mM 0.3243 mL 1.6214 mL 3.2428 mL 8.1069 mL
15 mM 0.2162 mL 1.0809 mL 2.1618 mL 5.4046 mL
20 mM 0.1621 mL 0.8107 mL 1.6214 mL 4.0534 mL
25 mM 0.1297 mL 0.6486 mL 1.2971 mL 3.2428 mL
30 mM 0.1081 mL 0.5405 mL 1.0809 mL 2.7023 mL
40 mM 0.0811 mL 0.4053 mL 0.8107 mL 2.0267 mL
50 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6214 mL
60 mM 0.0540 mL 0.2702 mL 0.5405 mL 1.3511 mL
80 mM 0.0405 mL 0.2027 mL 0.4053 mL 1.0134 mL
100 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.8107 mL
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Derenofylline 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:

Derenofylline251945-92-3SLV 320SLV320SLV-320Adenosine ReceptorP1 receptorNephrectomyfibrosisuraemiccardiomyopathynephrectomyInhibitorinhibitorinhibit

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