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Revefenacin

SKU: orb1299860

Description

Revefenacin (TD-4208) is a potent and selective long-acting muscarinic M3 receptor antagonist (Ki = 0.18 nM). It is a research compound investigated for chronic obstructive pulmonary disease (COPD), with studies demonstrating its bronchodilatory effects in both in vitro assays and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number864750-70-9
MW597.75
Purity96.66% (May vary between batches)
FormulaC35H43N5O4
SMILESCN(CCN1CCC(CC1)OC(=O)Nc1ccccc1-c1ccccc1)C(=O)c1ccc(CN2CCC(CC2)C(N)=O)cc1
TargetAChR
SolubilityDMSO:49 mg/mL (81.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.69 mM)

Bioactivity

Target IC50
M3 mAChR:0.18 Nm(ki)
In Vivo
In anesthetized dogs, Revefenacin, along with tiotropium and glycopyrronium, produced sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled Revefenacin exhibited dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency (expressed as concentration of dosing solution) was 45.0 μg/ml.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Inhibitor, GSK 1160724, GSK1160724, GSK-1160724, inhibit, Muscarinic acetylcholine receptor, mAChR, Revefenacin, TD 4208, TD4208, TD-4208

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Key Properties

No computed properties available.

Protocol Information

Available Sizes

Select a size below

1 mg
$ 80.00
5 mg
$ 130.00
1 ml x 10 mM (in DMSO)
$ 150.00
10 mg
$ 190.00
25 mg
$ 310.00
50 mg
$ 440.00
100 mg
$ 610.00
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