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MedKoo Cat#: 314250 | Name: Olodaterol free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Olodaterol, also known as BI 1744, is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim. Olodaterol was approved by FDA in 2014 for the treatment of chronic obstructive pulmonary disease.

Chemical Structure

Olodaterol free base
Olodaterol free base
CAS#868049-49-4 (free base)

Theoretical Analysis

MedKoo Cat#: 314250

Name: Olodaterol free base

CAS#: 868049-49-4 (free base)

Chemical Formula: C21H26N2O5

Exact Mass: 386.1842

Molecular Weight: 386.45

Elemental Analysis:

Price and Availability

Size Price Availability Quantity
50mg USD 850.00 2 Weeks
100mg USD 1,550.00 2 Weeks
200mg USD 2,950.00 2 Weeks
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Related CAS #
868049-49-4 (free base) 869477-96-3 (HCl)
Synonym
BI-1744; BI 1744; BI1744; Olodaterol; Striverdi
IUPAC/Chemical Name
(R)-6-hydroxy-8-(1-hydroxy-2-((1-(4-methoxyphenyl)-2-methylpropan-2-yl)amino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one
InChi Key
COUYJEVMBVSIHV-SFHVURJKSA-N
InChi Code
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
SMILES Code
O=C1COC2=C([C@@H](O)CNC(C)(C)CC3=CC=C(OC)C=C3)C=C(O)C=C2N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO.
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively).
In vitro activity:
Human bronchial epithelial brushing from patients with and without COPD were cultured into air-liquid interface (ALI) cultures and treated with or without olodaterol and RSV infection to examine the effect on markers of inflammation including interleukin-8 (IL-8) and mucus secretion. At baseline, COPD-ALIs produced greater amounts of IL-8 than control ALIs. Olodaterol reduced RSV-mediated IL-8 secretion in both COPD and control ALIs and also significantly reduced Muc5AC staining in COPD-ALIs infected with RSV. Reference: Respir Res. 2021 Feb 23;22(1):65. https://pubmed.ncbi.nlm.nih.gov/33622325/
In vivo activity:
The aim of this study was to test the efficacy of the long-acting β2-AR agonist olodaterol with regard to its antitussive property in a pre-clinical model of citric acid-induced cough in guinea pigs and to compare the results to different clinically relevant β2-AR agonists. Olodaterol dose-dependently inhibited the number of cough events in naïve and even more potently and with a greater maximal efficacy in ovalbumin-sensitized guinea pigs (p < 0.01). In conclusion, olodaterol, at doses eliciting bronchodilation, showed antitussive properties in a model of citric acid-induced cough in naïve and ovalbumin-sensitized guinea pigs. Reference: PLoS One. 2015 Mar 17;10(3):e0119953. https://pubmed.ncbi.nlm.nih.gov/25781609/
Solvent mg/mL mM
Solubility
DMF 20.0 51.75
DMF:PBS (pH 7.2) (1:3) 0.3 0.65
DMSO 46.0 119.03
Ethanol 20.5 53.05
Water 6.2 16.04
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 386.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Yang N, Singhera GK, Yan YX, Pieper MP, Leung JM, Sin DD, Dorscheid DR. Olodaterol exerts anti-inflammatory effects on COPD airway epithelial cells. Respir Res. 2021 Feb 23;22(1):65. doi: 10.1186/s12931-021-01659-2. PMID: 33622325; PMCID: PMC7901009. 2. Bouyssou T, Casarosa P, Naline E, Pestel S, Konetzki I, Devillier P, Schnapp A. Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models. J Pharmacol Exp Ther. 2010 Jul;334(1):53-62. doi: 10.1124/jpet.110.167007. Epub 2010 Apr 6. Erratum in: J Pharmacol Exp Ther. 2013 Jul;346(1):161. PMID: 20371707. 3. Herrmann FE, Wollin L, Wirth J, Gantner F, Lämmle B, Wex E. Olodaterol shows anti-fibrotic efficacy in in vitro and in vivo models of pulmonary fibrosis. Br J Pharmacol. 2017 Nov;174(21):3848-3864. doi: 10.1111/bph.13982. Epub 2017 Sep 20. PMID: 28810065; PMCID: PMC5647188. 4. Wex E, Bouyssou T. Olodaterol attenuates citric acid-induced cough in naïve and ovalbumin-sensitized and challenged guinea pigs. PLoS One. 2015 Mar 17;10(3):e0119953. doi: 10.1371/journal.pone.0119953. PMID: 25781609; PMCID: PMC4364307.
In vitro protocol:
1. Yang N, Singhera GK, Yan YX, Pieper MP, Leung JM, Sin DD, Dorscheid DR. Olodaterol exerts anti-inflammatory effects on COPD airway epithelial cells. Respir Res. 2021 Feb 23;22(1):65. doi: 10.1186/s12931-021-01659-2. PMID: 33622325; PMCID: PMC7901009. 2. Bouyssou T, Casarosa P, Naline E, Pestel S, Konetzki I, Devillier P, Schnapp A. Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models. J Pharmacol Exp Ther. 2010 Jul;334(1):53-62. doi: 10.1124/jpet.110.167007. Epub 2010 Apr 6. Erratum in: J Pharmacol Exp Ther. 2013 Jul;346(1):161. PMID: 20371707.
In vivo protocol:
1. Herrmann FE, Wollin L, Wirth J, Gantner F, Lämmle B, Wex E. Olodaterol shows anti-fibrotic efficacy in in vitro and in vivo models of pulmonary fibrosis. Br J Pharmacol. 2017 Nov;174(21):3848-3864. doi: 10.1111/bph.13982. Epub 2017 Sep 20. PMID: 28810065; PMCID: PMC5647188. 2. Wex E, Bouyssou T. Olodaterol attenuates citric acid-induced cough in naïve and ovalbumin-sensitized and challenged guinea pigs. PLoS One. 2015 Mar 17;10(3):e0119953. doi: 10.1371/journal.pone.0119953. PMID: 25781609; PMCID: PMC4364307.
1: O'Donnell DE, Casaburi R, Frith P, Kirsten A, De Sousa D, Hamilton A, Xue W, Maltais F. Effects of combined tiotropium/olodaterol on inspiratory capacity and exercise endurance in COPD. Eur Respir J. 2017 Apr 19;49(4). pii: 1601348. doi: 10.1183/13993003.01348-2016. Print 2017 Apr. PubMed PMID: 28424359. 2: Cataldo D. [Spiolto Respimat® : tiotropium-olodaterol fixed combination for therapy of chronic obstructive pulmonary disease (COPD)]. Rev Med Liege. 2016 Jun;71(6):308-313. Review. French. PubMed PMID: 28383865. 3: Ichinose M, Kato M, Takizawa A, Sakamoto W, Grönke L, Tetzlaff K, Fukuchi Y. Long-term safety and efficacy of combined tiotropium and olodaterol in Japanese patients with chronic obstructive pulmonary disease. Respir Investig. 2017 Mar;55(2):121-129. doi: 10.1016/j.resinv.2016.09.004. Epub 2016 Dec 22. PubMed PMID: 28274527. 4: Donohue JF, Betts KA, Du EX, Altman P, Goyal P, Keininger DL, Gruenberger JB, Signorovitch JE. Comparative efficacy of long-acting β2-agonists as monotherapy for chronic obstructive pulmonary disease: a network meta-analysis. Int J Chron Obstruct Pulmon Dis. 2017 Jan 19;12:367-381. doi: 10.2147/COPD.S119908. eCollection 2017. PubMed PMID: 28176892; PubMed Central PMCID: PMC5261557. 5: Ferguson GT, Karpel J, Bennett N, Clerisme-Beaty E, Grönke L, Voß F, Buhl R. Effect of tiotropium and olodaterol on symptoms and patient-reported outcomes in patients with COPD: results from four randomised, double-blind studies. NPJ Prim Care Respir Med. 2017 Dec;27(1):7. doi: 10.1038/s41533-016-0002-x. Epub 2017 Feb 2. PubMed PMID: 28154373. 6: Koblížek V, Svoboda M. [Current position of new fixed-dose combination of tiotropium and olodaterol - its role in the treatment of chronic obstructive pulmonary disease in the Czech Republic]. Vnitr Lek. 2016 Winter;62(12):1011-1020. Czech. PubMed PMID: 28139131. 7: Płusa T. [New bronchodilation treatment options for patients with COPD]. Pol Merkur Lekarski. 2017 Jan 23;42(247):5-12. Polish. PubMed PMID: 28134225. 8: Price D, Østrem A, Thomas M, Welte T. Dual bronchodilation in COPD: lung function and patient-reported outcomes - a review. Int J Chron Obstruct Pulmon Dis. 2016 Dec 30;12:141-168. doi: 10.2147/COPD.S116719. eCollection 2017. Review. PubMed PMID: 28115839; PubMed Central PMCID: PMC5221557. 9: An update on LAMA/LABA combinations for COPD. Drug Ther Bull. 2017 Jan;55(1):2-5. doi: 10.1136/dtb.2017.1.0451. Epub 2017 Jan 5. PubMed PMID: 28057707. 10: Derom E, Brusselle GG, Joos GF. Efficacy of tiotropium-olodaterol fixed-dose combination in COPD. Int J Chron Obstruct Pulmon Dis. 2016 Dec 13;11:3163-3177. doi: 10.2147/COPD.S92840. eCollection 2016. Review. PubMed PMID: 28008243; PubMed Central PMCID: PMC5167492. 11: Buhl R, Magder S, Bothner U, Tetzlaff K, Voß F, Loaiza L, Vogelmeier CF, McGarvey L. Long-term general and cardiovascular safety of tiotropium/olodaterol in patients with moderate to very severe chronic obstructive pulmonary disease. Respir Med. 2017 Jan;122:58-66. doi: 10.1016/j.rmed.2016.11.011. Epub 2016 Nov 14. PubMed PMID: 27993292. 12: Lee HW, Kim HJ, Lee CH. The impact of olodaterol on the risk of mortality and serious adverse events: a systematic review and meta-analysis. Br J Clin Pharmacol. 2016 Dec 13. doi: 10.1111/bcp.13210. [Epub ahead of print] PubMed PMID: 27957746. 13: Tamura T, Satoh H. Superiority of tiotropium plus olodaterol in comparison with salmeterol plus fluticasone. Int J Chron Obstruct Pulmon Dis. 2016 Nov 23;11:2909-2911. eCollection 2016. PubMed PMID: 27920517; PubMed Central PMCID: PMC5125986. 14: Tebboth A, Ternouth A, Gonzalez-Rojas N. UK-specific cost-effectiveness of tiotropium + olodaterol fixed-dose combination versus other LAMA + LABA combinations in patients with COPD. Clinicoecon Outcomes Res. 2016 Nov 7;8:667-674. eCollection 2016. PubMed PMID: 27853383; PubMed Central PMCID: PMC5106216. 15: Ferguson GT, Karpel JP, Clerisme-Beaty E, Grönke L, Voß F, Buhl R. Efficacy and safety of tiotropium + olodaterol maintenance treatment in patients with COPD in the TONADO(®) and OTEMTO(®) studies: a subgroup analysis by age. Int J Chron Obstruct Pulmon Dis. 2016 Oct 31;11:2701-2710. eCollection 2016. PubMed PMID: 27843306; PubMed Central PMCID: PMC5098524. 16: van Boven JF, Kocks JW, Postma MJ. Cost-effectiveness and budget impact of the fixed-dose dual bronchodilator combination tiotropium-olodaterol for patients with COPD in the Netherlands. Int J Chron Obstruct Pulmon Dis. 2016 Sep 19;11:2191-2201. eCollection 2016. PubMed PMID: 27703341; PubMed Central PMCID: PMC5036592. 17: Halpin DM, Kerkhof M, Soriano JB, Mikkelsen H, Price DB. Eligibility of real-life patients with COPD for inclusion in trials of inhaled long-acting bronchodilator therapy. Respir Res. 2016 Sep 23;17(1):120. PubMed PMID: 27663386; PubMed Central PMCID: PMC5034631. 18: Ichinose M, Taniguchi H, Takizawa A, Grönke L, Loaiza L, Voß F, Zhao Y, Fukuchi Y. The efficacy and safety of combined tiotropium and olodaterol via the Respimat(®) inhaler in patients with COPD: results from the Japanese sub-population of the Tonado(®) studies. Int J Chron Obstruct Pulmon Dis. 2016 Aug 29;11:2017-27. doi: 10.2147/COPD.S110389. eCollection 2016. PubMed PMID: 27621608; PubMed Central PMCID: PMC5010080. 19: Perriello EA, Sobieraj DM. The Respimat Soft Mist Inhaler, a Novel Inhaled Drug Delivery Device. Conn Med. 2016 Jun-Jul;80(6):359-64. Review. PubMed PMID: 27509644. 20: Selya-Hammer C, Gonzalez-Rojas Guix N, Baldwin M, Ternouth A, Miravitlles M, Rutten-van Mölken M, Goosens LM, Buyukkaramikli N, Acciai V. Development of an enhanced health-economic model and cost-effectiveness analysis of tiotropium + olodaterol Respimat® fixed-dose combination for chronic obstructive pulmonary disease patients in Italy. Ther Adv Respir Dis. 2016 Oct;10(5):391-401. doi: 10.1177/1753465816657272. Epub 2016 Jul 12. PubMed PMID: 27405723.