High Quality Ambrisentan CAS 177036-94-1 with best price and fast delivery

Ambrisentan More Info

Ambrisentan is an endothelin receptor antagonist (ERA) primarily used in the treatment of pulmonary arterial hypertension (PAH). It selectively targets the endothelin type A (ETA) receptors, leading to vasodilation and improved exercise capacity in affected patients.

Mechanism of Action

Ambrisentan works by blocking the action of endothelin-1 (ET-1), a potent vasoconstrictor that plays a significant role in the pathophysiology of PAH. The key mechanisms include:
Selective ETA Receptor Antagonism: By inhibiting ETA receptors, ambrisentan prevents ET-1 from causing vasoconstriction and cell proliferation in vascular smooth muscle. This leads to relaxation of blood vessels and a decrease in pulmonary artery pressure.
Preservation of ETB Receptor Function: Unlike non-selective ERAs, ambrisentan does not significantly inhibit ETB receptors, which mediate vasodilation and the clearance of ET-1. This selectivity helps maintain some beneficial vascular functions while reducing harmful effects associated with increased ET-1 levels.

Applications

Pulmonary Arterial Hypertension: It is approved for use as a single agent or in combination with tadalafil to improve exercise ability, delay clinical worsening, and reduce hospitalization risks in patients with PAH. Clinical studies have shown its efficacy in both idiopathic and heritable forms of PAH, as well as PAH associated with connective tissue diseases.

Routes of Administration

Ambrisentan is administered orally, typically available in tablet form at doses of 5 mg and 10 mg. It can be taken with or without food, and absorption is not significantly affected by dietary intake.

Safety and Side Effects

While generally well-tolerated, ambrisentan can cause several side effects:
Common Side Effects
Peripheral edema (swelling of limbs)
Nasal congestion
Flushing
Headache
Abdominal pain
Serious Side Effects
Patients should seek immediate medical attention if they experience:
Signs of liver problems (e.g., dark urine, jaundice)
Severe shortness of breath or chest pain
Rapid weight gain or swelling
Symptoms of anemia (e.g., pale skin, unusual tiredness).

Pharmacokinetics

Absorption: Rapidly absorbed with peak plasma concentrations occurring approximately 2 hours after oral administration. The absolute bioavailability is unknown but is consistent across doses within the therapeutic range.
Distribution: Highly protein-bound (99%), primarily to albumin. The mean blood-to-plasma ratio indicates limited distribution into red blood cells.
Metabolism: Primarily metabolized through glucuronidation by uridine 5’-diphosphate glucuronosyltransferases (UGTs) and to a lesser extent by cytochrome P450 enzymes (CYP3A4, CYP3A5).
Elimination: Mainly eliminated via non-renal pathways; approximately 22% of an administered dose is recovered in urine, with only about 3.3% excreted as unchanged drug. The remaining metabolites are primarily found in feces.
Half-Life: The elimination half-life ranges from 9 to 15 hours, allowing for once-daily dosing regimens.

Package Image

FAQ

Q1. Can I get a free sample?

We can send you a samll free sample, and you only need to pay for the shipping cost.

Q2. What is the HyperChem payment term?

T/T in advance
LC at sight
DP at sight

Bank transfer

PayPal

Bitcoin...

Q3. What is HyperChem shipment policy?

Our policy is to strive for the quickest shipment time possible.

For ready stock samples, they are usually shipped within 3 working days after payment received.
For non-ready stock, please contact HyperChem sales team to negotiate.

Q4. What is HyperChem shipment term?

By Express  
FedEx  UPS  DHL  EMS                               
Fast: 3-7 days around, high cost, door to door service

By Air                                        
Suitable for more than 50kg 
Fast: 3-7 days, hight cost, port to port, professional broker needed 

By Sea
Suitable for more than 500kg      
Fast: 7-45 days, low cost, port to port, professional broker needed 

We will always attempt to utilize the quickest and most affordable way for customers to receive orders. And follow -up with customers via email for all shipment details as well as updated track information until it arrives without damage.

Q5. What HyperChem will provide after shipment?

For sample orders: 
After shipment is done, an timely email including:

1. Track details (Fedex /TNT/DHL/EMS Track number)
2. Packaging photo
3. COA, MSDS, etc
4. Dispatch date & Estimated arriving time
5. Shipping invoice

For commercial orders
A full set of shipment documents as well as package photos can be provided in scan-copy and original, to help customers complete the customs clearance process.

Company Profile

Established in 2013, Hyper Chem has exclusive tie-ups with leading manufacturers, supplying raw materials produced in GMP and ISO 9002 certified facilities, and provides high-quality ingredients and raw materials to cater to the requirements of our diverse range of clients.

Among them, our key client industrial sectors around the global are:

Pharmaceuticals
Nutrition Ingredients/ Dietary supplements
Cosmetic Ingredients
Food Ingredients
Veterinary API
Agriculture fertilizer
Custom Synthesis lab supply

HyperChem provides to its wonderful and honorable clients comprehensive purchasing and distribution services which ensure that we are delivering the right generic, raw, or customized product, make sure that we are delivering it at the right time, ensure that it is delivered in the specified amount, and in the right kind of packaging to clients and customers of all types of industries irrespective of their size of operation.