AMG-548 dihydrochloride

Name: AMG-548 dihydrochloride
Brand: MedChemExpress
SKU: HY-108642B
Rating: 4.5 (1 reviews)

Cat. No.: HY-108642B Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

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

AMG-548 dihydrochloride Chemical Structure

CAS No. : 2518299-32-4

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 317	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 317	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2350	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AMG-548 dihydrochloride:

AMG-548 Get quote
AMG-548 hydrochloride Get quote

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All p38 MAPK Isoform Specific Products:

View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All Casein Kinase Isoform Specific Products:

View All Isoforms

CK1 CK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM)^[1]. AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε^[2].

IC₅₀ & Target^[1]^[2]

p38α

0.5 nM (Ki)

p38β

3.6 nM (Ki)

p38δ

2600 nM (Ki)

p38γ

4100 nM (Ki)

dog p38α

5.0 nM (Ki)

JNK 1

11480 nM (Ki)

JNK 2

39 nM (Ki)

JNK 3

61 nM (Ki)

CK1

In Vitro

AMG-548 dihydrochloride shows >1000 fold selective against p38γ (K_i=2600 nM) and p38δ (k_i=4100 nM). AMG-548 dihydrochloride has an modest selectivity against JNK2 (k_i=39 nM) and JNK3 (k_i=61 nM). AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC₅₀=3 nM) and IL1b (IC₅₀=7 nM) as well as TNFa induced IL-8 (IC₅₀=0.7 nM) and IL-1b induced IL-6 (IC50₅₀=1.3 nM) in human whole blood^[1].
AMG-548 dihydrochloride (10 μM) inhibits the hDvl2 shift^[2].

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

In Vivo

AMG-548 dihydrochloride has rat F of 62% and dog F of 47%. The t_1/2 is 4.6 hours in rats and 7.3 hours in dogs^[1].

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

Molecular Weight

534.48

Formula

C₂₉H₂₉Cl₂N₅O

CAS No.

2518299-32-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C)C(NCC(N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (18.71 mM; ultrasonic and warming and heat to 60°C; 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	1.8710 mL	9.3549 mL	18.7098 mL
5 mM	0.3742 mL	1.8710 mL	3.7420 mL
10 mM	0.1871 mL	0.9355 mL	1.8710 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). 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)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.87 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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)

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).

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

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: 99.91%

Select Batch:

Data Sheet (277 KB) SDS (420 KB)

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94. [Content Brief]

[2]. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8710 mL	9.3549 mL	18.7098 mL	46.7744 mL
	5 mM	0.3742 mL	1.8710 mL	3.7420 mL	9.3549 mL
	10 mM	0.1871 mL	0.9355 mL	1.8710 mL	4.6774 mL
	15 mM	0.1247 mL	0.6237 mL	1.2473 mL	3.1183 mL