Olodaterol - CAS 868049-49-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H26N2O5
Molecular Weight:
386.44
COA:
Inquire
Targets:
Adrenergic Receptor
Description:
Olodaterol, also referred to BI1744, is a long acting β2-agonist (β2-ARs; EC50s = 97.7 and 2,725 nM for human β2- and β1-ARs, respectively) used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim.
Brife Description:
A long acting beta-adrenoceptor agonist (EC50= 1.4±0.08 Nm)
Related CAS:
869477-96-3 (HCl)
Synonyms:
6-hydroxy-8-[(1R)-1-hydroxy-2-[[1-(4-methoxyphenyl)-2-methylpropan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one; 6-hydroxy-8-(1-hydroxy-2-((2-(4-methoxyphenyl)-1,1-dimethylethyl)amino)ethyl)-2H-1,4-benzoxazin-3(4H)-one; BI 1744 CL; BI-1744 CL; olodaterol; Striverdi; Respimat
Solubility:
H2O: 6.2 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
649.0±55.0 ℃ at 760 Torr
Density:
1.250±0.06 g/cm3
InChIKey:
COUYJEVMBVSIHV-SFHVURJKSA-N
InChI:
1S/C21H26N2O5/c1-21(2,10-13-4-6-15(27-3)7-5-13)22-11-18(25)16-8-14(24)9-17-20(16)28-12-19(26)23-17/h4-9,18,22,24-25H,10-12H2,1-3H3,(H,23,26)/t18-/m0/s1
Canonical SMILES:
CC(C)(CC1=CC=C(C=C1)OC)NCC(C2=CC(=CC3=C2OCC(=O)N3)O)O
1.Efficacy of tiotropium-olodaterol fixed-dose combination in COPD.
Derom E;Brusselle GG;Joos GF Int J Chron Obstruct Pulmon Dis. 2016 Dec 13;11:3163-3177. doi: 10.2147/COPD.S92840. eCollection 2016.
Tiotropium-olodaterol, formulated in the Respimat soft-mist inhaler, is an inhaled fixed-dose combination (FDC) of a long-acting muscarinic antagonist (LAMA) and a long-acting β;2;-agonist (LABA), commercialized under the name of Spiolto or Stiolto. The efficacy of tiotropium-olodaterol 5-5 μg once daily in adult patients with COPD was documented in eleven large, multicenter trials of up to 52 weeks duration. Tiotropium-olodaterol 5-5 μg not only improved spirometric values to a significantly greater extent than placebo but also resulted in statistically significant beneficial effects on dyspnea, markers of hyperinflation, use of rescue medication, health-related quality of life, and exercise endurance. Improvements exceeded the minimal clinically important difference (MCID) for forced expiratory volume in 1 second (FEV;1;), dyspnea, and quality of life. Differences between tiotropium-olodaterol 5-5 μg and the respective monocomponents were statistically significant for FEV;1;, dyspnea, markers of hyperinflation, use of rescue medication, and health-related quality of life, but did not reach the MCID. However, dual bronchodilatation significantly increased the number of patients who exceeded the MCID for dyspnea and quality of life.
2.Bronchodilating drugs for chronic obstructive pulmonary disease: current status and future trends.
Montuschi P;Ciabattoni G J Med Chem. 2015 May 28;58(10):4131-64. doi: 10.1021/jm5013227. Epub 2015 Feb 9.
Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting β2-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide are administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration. New once-daily LABA, including vilanterol, olodaterol, milveterol, carmoterol, and abediterol, are in development. LAMA/LABA fixed dose combinations (FDCs) provide the convenience of two bronchodilators with different mechanism of action in a single inhaler. Indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium FDCs have been approved or are under approval and are likely to become a standard pharmacological strategy for COPD. Inhaled dual-pharmacology compounds, combining muscarinic antagonism and β2-agonism (MABA) in a single molecule, potentially provide additive or synergistic bronchodilation over either inhaled antimuscarinic or β2-agonist monotherapy.
3.Clinicopharmacological profile of the fixed-dose combination of aclidinium bromide and formoterol fumarate in the management of chronic obstructive pulmonary disease.
Babu KS;Morjaria JB Ther Adv Respir Dis. 2015 Apr;9(2):56-68. doi: 10.1177/1753465815575254. Epub 2015 Mar 9.
The recent Global Initiative for Chronic Obstructive Lung Disease (GOLD) chronic obstructive pulmonary disease (COPD) guidelines consider symptoms and exacerbation history in addition to the degree of airflow obstruction for classifying patients. The improvement of symptoms is principally provided by bronchodilators, using β2 agonists and antimuscarinic agents. Aclidinium bromide is a novel long-acting antimuscarinic agent licensed for use in patients with COPD. Novel fixed-dose combinations that are either licensed or in their late phase of development include vilanterol/umeclidinium, indacaterol/glycopyrronium, olodaterol/tiotropium and formoterol/aclidinium. Fixed-dose combinations of aclidinium/formoterol have been evaluated in COPD patients and evidence suggests that this is efficacious, safe, has a quick onset of action and is well tolerated. This review provides a clinico-pharmacological profile of this compound.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Adrenergic Receptor Products


CAS 108929-47-1 CGP-12388

CGP-12388
(CAS: 108929-47-1)

CGP-12388 is a beta-adrenoceptor antagonist-derived radioligands. It is used for cardiac PET imaging due to its high hydrophilicity and affinity to beta-adrenoc...

CAS 72795-01-8 ICI 118551 hydrochloride

ICI 118551 hydrochloride
(CAS: 72795-01-8)

ICI 118551 hydrochloride is a highly selective β2 adrenergic antagonist (Ki values are 1.2, 120 and 257 nM for β2, β1 and β3 receptors respectively), inhibited ...

CAS 5053-08-7 Fenspiride Hydrochloride

Fenspiride Hydrochloride
(CAS: 5053-08-7)

Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 ...

CAS 89365-50-4 Salmeterol

Salmeterol
(CAS: 89365-50-4)

Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist. It is used clinically in the maintenance and prevention of asthma symptoms and mainten...

Colterol acetate
(CAS: 10255-14-8)

Colterol acetate is a short-acting β2-adrenoreceptor agonist. Bitolterol is the prodrug of Colterol used for the treatment of asthma and chronic obstructive pul...

CAS 94-07-5 Synephrine

Synephrine
(CAS: 94-07-5)

Synephrine is an α-adrenergic receptor agonist used as a vasoconstrictor.

CAS 29122-68-7 Atenolol

Atenolol
(CAS: 29122-68-7)

Atenolol, with antianginal and antiarrhythmic properties, it is a cardioselective beta-adrenergic blocker and used in hypertension control.

CAS 318-98-9 Propranolol Hydrochloride

Propranolol Hydrochloride
(CAS: 318-98-9)

Propranolol hydrochloride, with antihypertensive, antianginal and antiarrhythmic (class II) properties, is a non-cardioselective adrenergic-beta antagonist and ...

CAS 208993-54-8 Fiduxosin

Fiduxosin
(CAS: 208993-54-8)

Fiduxosin is a potent antagonist of α1-adrenoceptor, with Ki= 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively. Fiduxosin was...

CAS 76631-46-4 Detomidine

Detomidine
(CAS: 76631-46-4)

Detomidine is an imidazole derivative and a α2-adrenergic agonist. It is usually used in the form of detomidine hydrochloride. It is used as a large animal seda...

CAS 53671-71-9 ICI 89406

ICI 89406
(CAS: 53671-71-9)

ICI 89406 is a selective β-adrenergic antagonist. It is a low efficacy partial agonist and does not affect resting cardiac parameters.

CAS 63590-64-7 Terazosin

Terazosin
(CAS: 63590-64-7)

Terazosin, works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls, is a selective alpha1-antagonist used for trea...

CAS 30007-39-7 HEAT hydrochloride

HEAT hydrochloride
(CAS: 30007-39-7)

HEAT hydrochloride is a selective α1-adrenoceptor antagonist, precursor to the 3-[125I]-derivative.

BMS-196085
(CAS: 170686-10-9)

BMS-196085, a sulfanilamide derivative, has been found to be a β-adrenergic receptor agonist that was once studied in obesity as well as yype 2 diabetes mellitu...

CAS 158599-53-2 Zoleprodolol

Zoleprodolol
(CAS: 158599-53-2)

Zoleprodolol, an oxadiazol derivative, has been found to be an adrenergic receptor antagonist.

CAS 312753-06-3 Indacaterol

Indacaterol
(CAS: 312753-06-3)

Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.

CAS 214548-46-6 Lusaperidone

Lusaperidone
(CAS: 214548-46-6)

Lusaperidone, also known as R107474, is an α2 adrenergic receptor antagonist. R107474 showed high affinity for ha2A-, ha2B-, and ha2C-adrenoceptors, stably expr...

CP 59430
(CAS: 86329-06-8)

CP 59430 is an azide analog of prazosin. It is a selective alpha 1-adrenergic receptor antagonist.

CAS 81167-22-8 Imiloxan hydrochloride

Imiloxan hydrochloride
(CAS: 81167-22-8)

Imiloxan hydrochloride is the hydrochloride salt of imiloxan, which is a moderately potent and highly selective α2-adrenoceptor antagonist. It shows no affinity...

ABT-866
(CAS: 258526-74-8)

ABT-866 is a novel alpha-adrenoceptor agent that demonstrates intrinsic activity at the α1A-adrenoceptor subtype present in the rabbit urethra (pD2=6.22, with 8...

Chemical Structure

CAS 868049-49-4 Olodaterol

Quick Inquiry

Verification code

Featured Items