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Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage. Inflachromene can be used for the research of neuroinflammatory disorders.

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

Inflachromene Chemical Structure

Inflachromene Chemical Structure

CAS No. : 908568-01-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 560 In-stock
25 mg USD 1120 In-stock
50 mg USD 1600 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage. Inflachromene can be used for the research of neuroinflammatory disorders[1][2].

IC50 & Target

HMGB[2]

In Vitro

Inflachromene (0.01-100 μM; 24 h) efficiently blocks LPS-induced nitrite release in a dose-dependent manner without any toxicity in BV-2 microglial cells[2].
Inflachromene (1-10 μM) suppresses the increased levels of inflammation-related genes, such as Il6, Il1b, Nos2 and Tnf, after LPS stimulation[2].
Inflachromene (5 μM) reduces LPS-induced secretion of the proinflammatory cytokine TNF-α[2].
Inflachromene (5 μM; 30 min) substantially suppresses the nuclear translocation of NF-κB and the degradation of IκB[2].
Inflachromene (1-10 μM; 30 min) inhibits LPS-induced phosphorylation of ERK, JNK and p38 MAPK in microglia[2].
Inflachromene (10 μM; 30 min) completely prevents the death of cocultured neuroblastoma and primary neuronal cells by inhibiting microglia-mediated neurotoxicity[2].
Inflachromene (1-10 μM; 24 h) has no significant effect on the viability of neurons[2].

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

In Vivo

Inflachromene (2-10 mg/kg; i.p. once daily for 4 days) effectively blocks LPS-mediated microglial activation[2].
Inflachromene (10 mg/kg; i.p. once daily for 30 days) significantly reduces the progression of disease, as determined by EAE clinical score[2].
Inflachromene (1 mg/kg; i.v.) exhibits long half-life (14.1±6.43 h) and moderate Vss (2.02±1.02 L/kg)[1].
Inflachromene (1 mg/kg; p.o.) exhibits high oral bioavailability (94%) and Cmax (0.59±0.16 g/mL)[1].

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

Animal Model: Male C57BL/6 mice (11 weeks; 25-30 g) are treated with LPS[2]
Dosage: 2, 10 mg/kg
Administration: I.p. once daily for 4 days
Result: Blocked LPS-mediated microglial activation, even at a dose of 2 mg/kg.
Animal Model: Sprague-Dawley (SD) rats (7 weeks; 230-250 g)[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. and p.o. administration
Result: I.v.: t1/2=14.1±6.43 h; CL= 0.14±0.01 L/kg/h; Vss=2.02±1.02 L/kg.
P.o.: t1/2=7.96±1.16 h; F=94%; Cmax=0.59±0.16 g/mL.
Molecular Weight

377.39

Formula

C21H19N3O4

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N(C2=CC=CC=C2)C(N3CC=C(C(C)(C)OC4=CC(O)=CC=C45)C5N31)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (264.98 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 2.6498 mL 13.2489 mL 26.4978 mL
5 mM 0.5300 mL 2.6498 mL 5.2996 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (6.62 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 (6.62 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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Dosing volume
(per animal)

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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.88%

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 (sealed storage, away from moisture and light). 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 2.6498 mL 13.2489 mL 26.4978 mL 66.2445 mL
5 mM 0.5300 mL 2.6498 mL 5.2996 mL 13.2489 mL
10 mM 0.2650 mL 1.3249 mL 2.6498 mL 6.6244 mL
15 mM 0.1767 mL 0.8833 mL 1.7665 mL 4.4163 mL
20 mM 0.1325 mL 0.6624 mL 1.3249 mL 3.3122 mL
25 mM 0.1060 mL 0.5300 mL 1.0599 mL 2.6498 mL
30 mM 0.0883 mL 0.4416 mL 0.8833 mL 2.2081 mL
40 mM 0.0662 mL 0.3312 mL 0.6624 mL 1.6561 mL
50 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3249 mL
60 mM 0.0442 mL 0.2208 mL 0.4416 mL 1.1041 mL
80 mM 0.0331 mL 0.1656 mL 0.3312 mL 0.8281 mL
100 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6624 mL
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Inflachromene 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.

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