AHR antagonist 5 free base

Name: AHR antagonist 5 free base
Brand: MedChemExpress
SKU: HY-141609
Rating: 4.5 (1 reviews)

Cat. No.: HY-141609 Purity: 99.56%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.

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

AHR antagonist 5 free base Chemical Structure

CAS No. : 2247950-42-9

Size	Price	Stock	Quantity
1 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AHR antagonist 5 free base:

AHR antagonist 5 In-stock
AHR antagonist 5 hemimaleate Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

AHR antagonist 5 free base (Compound A) potently inhibits AHR activity in human and rodent cell lines (IC₅₀ of ~35-150 nM). In human T cell assays, AHR antagonist 5 free base induces an activated T cell state. AHR antagonist 5 free base inhibits CYP1A1 and interleukin (IL)-22 gene expression and leads to an increase in pro-inflammatory cytokines, such as IL-2 and IL-9^[1].

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

In Vivo

AHR antagonist 5 free base (Compound A) has been evaluated in a series of pharmacological, single-dose and repeated-dose toxicological studies in rodent and non-rodent species including 28-day Good Laboratory Practice (GLP) studies in rat and monkeys. All changes are resolved or resolving after 2 weeks of dosing cessation, except for the testicular changes in rats^[1].

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

Molecular Weight

441.50

Formula

C₂₅H₂₄FN₇

CAS No.

2247950-42-9

Appearance

Solid

Color

White to off-white

SMILES

CC(C)C(C=N1)=C2N1C(N[C@H]3CC4=C(CC3)NC5=CC=CC=C45)=NC(C6=CN=CC(F)=C6)=N2

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 (226.50 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	2.2650 mL	11.3250 mL	22.6501 mL
5 mM	0.4530 mL	2.2650 mL	4.5300 mL
10 mM	0.2265 mL	1.1325 mL	2.2650 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.66 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)

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: 99.56%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (256 KB) HNMR (115 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Marta Sanchez-Martin, et al. Ahr inhibitors and uses thereof. WO2021142180A1.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2650 mL	11.3250 mL	22.6501 mL	56.6251 mL
	5 mM	0.4530 mL	2.2650 mL	4.5300 mL	11.3250 mL
	10 mM	0.2265 mL	1.1325 mL	2.2650 mL	5.6625 mL
	15 mM	0.1510 mL	0.7550 mL	1.5100 mL	3.7750 mL
	20 mM	0.1133 mL	0.5663 mL	1.1325 mL	2.8313 mL
	25 mM	0.0906 mL	0.4530 mL	0.9060 mL	2.2650 mL
	30 mM	0.0755 mL	0.3775 mL	0.7550 mL	1.8875 mL
	40 mM	0.0566 mL	0.2831 mL	0.5663 mL	1.4156 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1325 mL
	60 mM	0.0378 mL	0.1888 mL	0.3775 mL	0.9438 mL
	80 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
	100 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5663 mL