Ambrisentan (Synonyms: BSF 208075; LU 208075)

Name: Ambrisentan
Brand: MedChemExpress
SKU: HY-13209
Rating: 4.5 (2 reviews)

Cat. No.: HY-13209 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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Ambrisentan is a selective ET type A receptor (ETAR) antagonist.

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

Ambrisentan Chemical Structure

CAS No. : 177036-94-1

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Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 251	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 383	In-stock	Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

Other Forms of Ambrisentan:

Ambrisentan sodium Get quote
Ambrisentan-d₁₀ Get quote

2 Publications Citing Use of MCE Ambrisentan

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Protocol
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Description

Ambrisentan is a selective ET type A receptor (ETAR) antagonist.

IC₅₀ & Target

ETA receptor^[1]

In Vitro

Ambrisentan is an endothelin type A receptor antagonist^[1]. Ambrisentan induces Nrf2 activation. Endothelial permeability increased in BMEC monolayers at 24 h of hypoxia exposure and compared to vehicle control, Ambrisentan attenuates hypoxia-induced BMEC leak. These results are reversed when prior to treatment BMEC are transfected with siRNA against Nrf2^[2].

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

In Vivo

In the Ambrisentan group, hepatic hydroxyproline content is significantly lower than in the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). Moreover, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis^[1].

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

Clinical Trial

Molecular Weight

378.42

Formula

C₂₂H₂₂N₂O₄

CAS No.

177036-94-1

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H](C(OC)(C1=CC=CC=C1)C2=CC=CC=C2)OC3=NC(C)=CC(C)=N3)O

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 (264.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 7.14 mg/mL (18.87 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6426 mL	13.2128 mL	26.4257 mL
5 mM	0.5285 mL	2.6426 mL	5.2851 mL
10 mM	0.2643 mL	1.3213 mL	2.6426 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)

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: ≥ 2.5 mg/mL (6.61 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.61 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.
Protocol 3

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (7.1 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 4

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (7.1 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.
Protocol 5

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 0.71 mg/mL (1.88 mM); Clear solution

This protocol yields a clear solution of ≥ 0.71 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 EtOH stock solution (7.1 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (33.03 mM); Suspended solution; Need ultrasonic

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: 99.95%

Select Batch:

Data Sheet (284 KB) SDS (0 KB)

COA (256 KB) HNMR (271 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Okamoto T, et al. Antifibrotic effects of Ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model. World J Hepatol. 2016 Aug 8;8(22):933-41. [Content Brief]

[2]. Lisk C, et al. Nrf2 activation: a potential strategy for the prevention of acute mountain sickness. Free Radic Biol Med. 2013 Oct;63:264-73. [Content Brief]

Cell Assay ^[2]	Unless otherwise stated, for each BMEC experiment cells are randomly divided into 4 groups: (1) normoxia vehicle control (Nx-CTRL); (2) normoxia-treated; (3) hypoxia (24 h) control (Hx-CTRL) and (4) hypoxia (24 h) treated. As previously described, Nrf2 activators are added 24 h prior to any hypoxic exposures. Cell treatments are; Protandim (100 μg/mL), methazolamide (125 μg/mL, nifedipine (7 μg/mL) or Ambrisentan (40 μg/mL). In addition, some cells are treated with Nrf2 siRNA. In these experiments, siRNA is added 24 h prior to drug treatments. The rationale for 24 h hypoxia exposure for BMEC is to ensure that cells remained transfected with siRNA for the pre-treatment of drugs (24 h in normoxia) and during the 24 h hypoxia exposure. Data is collected from at least three separate cell culture preparations on three separate days (n=9)^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] A total of 13 male FLS-ob/ob mice (age, 8 wk; body weight, 42.88 g±1.74 g) are used. At the age of 12 wk, male FLS-ob/ob mice are randomly assigned to the Ambrisentan (n=8) or control (n= 5) group. Intragastric gavage administration is carried out in conscious animals with an appropriately sized gastric tube. Ambrisentan (2.5 mg/kg per day) is orally administered every afternoon for 4 wk as a bolus through a gastric tube. Water is administered to the control group. At week 4, animals are fasted for 4 h and tail vein blood is drawn and subjected to blood glucose determination. Animals are killed by pentobarbital anesthesia injection after 4 wk and blood is collected from the right ventricle. Plasma samples are frozen and stored at -80°C Liver and visceral fat are then weighed, snap-frozen in liquid nitrogen, and stored at -80°C. Additional liver specimens are fixed in 10% buffered formalin and embedded in paraffin for histological analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Okamoto T, et al. Antifibrotic effects of Ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model. World J Hepatol. 2016 Aug 8;8(22):933-41. [Content Brief] [2]. Lisk C, et al. Nrf2 activation: a potential strategy for the prevention of acute mountain sickness. Free Radic Biol Med. 2013 Oct;63:264-73. [Content Brief]

Complete Stock Solution Preparation Table

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

Ethanol / DMSO	1 mM	2.6426 mL	13.2128 mL	26.4257 mL	66.0642 mL
	5 mM	0.5285 mL	2.6426 mL	5.2851 mL	13.2128 mL
	10 mM	0.2643 mL	1.3213 mL	2.6426 mL	6.6064 mL
	15 mM	0.1762 mL	0.8809 mL	1.7617 mL	4.4043 mL
DMSO	20 mM	0.1321 mL	0.6606 mL	1.3213 mL	3.3032 mL
	25 mM	0.1057 mL	0.5285 mL	1.0570 mL	2.6426 mL
	30 mM	0.0881 mL	0.4404 mL	0.8809 mL	2.2021 mL
	40 mM	0.0661 mL	0.3303 mL	0.6606 mL	1.6516 mL
	50 mM	0.0529 mL	0.2643 mL	0.5285 mL	1.3213 mL
	60 mM	0.0440 mL	0.2202 mL	0.4404 mL	1.1011 mL
	80 mM	0.0330 mL	0.1652 mL	0.3303 mL	0.8258 mL
	100 mM	0.0264 mL	0.1321 mL	0.2643 mL	0.6606 mL

Ambrisentan 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:

Ambrisentan177036-94-1BSF 208075 LU 208075BSF208075BSF-208075LU208075LU 208075LU-208075Endothelin ReceptorInhibitorinhibitorinhibit

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Ambrisentan (Synonyms: BSF 208075; LU 208075)

Customer Review

Other Forms of Ambrisentan:

Ambrisentan Related Antibodies

2 Publications Citing Use of MCE Ambrisentan

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ambrisentan Related Antibodies

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Complete Stock Solution Preparation Table

Ambrisentan Related Classifications

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