2. Immunology/Inflammation
  3. IRAK
  4. HS271

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

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HS271 Chemical Structure

HS271 Chemical Structure

CAS No. : 2410393-15-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

HS271 Related Antibodies

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IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties[1].

IC50 & Target[1]

IRAK4

7.2 μM (IC50)

In Vivo

HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis[1].
HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL[1].
HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human[1].
HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively[1].

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

Animal Model: A rat model of collagen induced arthritis (CIA)[1].
Dosage: 15, 50, 150 mg/kg.
Administration: PO, once daily.
Result: Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
Molecular Weight

435.44

Formula

C21H24F3N5O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1=CC2=CN(CCN(C)C)N=C2C=C1C(C)(O)C)C3=NC(C(F)(F)F)=CC=C3
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 (229.65 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 2.2965 mL 11.4826 mL 22.9653 mL
5 mM 0.4593 mL 2.2965 mL 4.5931 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
=
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: ≥ 2.5 mg/mL (5.74 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 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: ≥ 2.5 mg/mL (5.74 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:

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
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 2.2965 mL 11.4826 mL 22.9653 mL 57.4132 mL
5 mM 0.4593 mL 2.2965 mL 4.5931 mL 11.4826 mL
10 mM 0.2297 mL 1.1483 mL 2.2965 mL 5.7413 mL
15 mM 0.1531 mL 0.7655 mL 1.5310 mL 3.8275 mL
20 mM 0.1148 mL 0.5741 mL 1.1483 mL 2.8707 mL
25 mM 0.0919 mL 0.4593 mL 0.9186 mL 2.2965 mL
30 mM 0.0766 mL 0.3828 mL 0.7655 mL 1.9138 mL
40 mM 0.0574 mL 0.2871 mL 0.5741 mL 1.4353 mL
50 mM 0.0459 mL 0.2297 mL 0.4593 mL 1.1483 mL
60 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9569 mL
80 mM 0.0287 mL 0.1435 mL 0.2871 mL 0.7177 mL
100 mM 0.0230 mL 0.1148 mL 0.2297 mL 0.5741 mL
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HS271 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:

HS2712410393-15-4HS 271HS-271IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseArthritisCIATNFαInhibitorinhibitorinhibit

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