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Olodaterol HCl, the hydrochloride salt of Olodaterol (BI-1744; BI1744; STRIVERDI RESPIMAT), is a ultra-long acting β-adrenergic receptor agonist approved in 2014 as an inhalation for the treatment of patients with chronic obstructive pulmonary disease (COPD).
| ln Vitro |
Olodaterol (0.001~10 nM; fibroblasts) hydrochloride initiates growth factor-induced motility and proliferation [2]. Olodaterol (0.1~10 nM; fibroblasts) hydrochloride interferes with FGF-induced phosphorylation of the signaling cascade [2]. Olodaterol (0.001~1000). nM; 30 min; fibroblasts) hydrochloric acid concentration raises intracellular cAMP in a dependent manner. Olodaterol (0 to 10 nM; 30 minutes; fibroblasts) hydrochloric acid concentration reduces the increase in PICP, with maximal effectiveness at 10 nM. Olodaterol hydrochloride exhibits subnanomolar affinity for β2-AR (pKi=9.14 ), olodaterol hydrochloride is selective for this receptor compared with β1-AR and β3-AR subtypes [2].
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| ln Vivo |
Olodaterol hydrochloride (1 mg/kg; inhalation; day 21) accelerates weight return to control levels (day 21) and attenuates TGF-β-induced pulmonary fibrosis [2]. Olodaterol (0.1 to 3 μg/kg; inhalation; Olodaterol (0.3 and 0.6 μg/kg; inhalation; 24 hours)) induces approximately 60% anesthetic protection after 0.5 hours [3].
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| Cell Assay |
Western Blot analysis [2]
Cell Types: fibroblasts Tested Concentrations: 0.1~10 nM Incubation Duration: Experimental Results: Interference with FGF-induced signaling cascade phosphorylation. Cell proliferation analysis[2] Cell Types: Fibroblasts Tested Concentrations: 0.001~10 nM Incubation Duration: Experimental Results: Growth factor-induced motility and proliferation were attenuated. |
| Animal Protocol |
Animal/Disease Models: Pulmonary fibrosis C57BL/6 mice
Doses: 1 mg/mL Route of Administration: inhalation; 21-day Experimental Results: Accelerated body weight recovery to control level (day 21) and attenuated TGF-β-induced pulmonary fibrosis. Animal/Disease Models: guinea pig Doses: 0.1~3 μg/kg Route of Administration: inhalation; 5 hrs (hrs (hours)) Experimental Results: Induced dose-dependent bronchial protection. Animal/Disease Models: Dog Doses: 0.3 and 0.6 μg/kg Route of Administration: Inhalation; 24 hrs (hrs (hours)) Experimental Results: Olodaterol (0.6 μg/kg) induced approximately 60% of maximal bronchial protection after 0.5 hrs (hrs (hours)). |
| References |
[1]. Xing G, et al. Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β2-adrenoceptor agonists. Bioorg Med Chem. 2020;28(1):115178.
[2]. Herrmann FE, et al. Olodaterol shows anti-fibrotic efficacy in in vitro and in vivo models of pulmonary fibrosis. Br J Pharmacol. 2017;174(21):3848-3864. [3]. Bouyssou T, et al. Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models [published correction appears in J Pharmacol Exp Ther. 2013 Jul;346(1):161]. J Pharmacol Exp Ther. 2010;334(1):53-62. |
| Molecular Formula |
C21H27CLN2O5
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|---|---|
| Molecular Weight |
422.906
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| CAS # |
869477-96-3
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| Related CAS # |
Olodaterol;868049-49-4
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| SMILES |
Cl.COC1=CC=C(CC(NC[C@@H](C2=C3C(NC(CO3)=O)=CC(O)=C2)O)(C)C)C=C1
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| Synonyms |
Olodaterol hydrochloride BI 1744 BI1744BI-1744 Olodaterol StriverdiOlodaterol HCl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~250 mg/mL (~591.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 14.29 mg/mL (33.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3646 mL | 11.8228 mL | 23.6457 mL | |
| 5 mM | 0.4729 mL | 2.3646 mL | 4.7291 mL | |
| 10 mM | 0.2365 mL | 1.1823 mL | 2.3646 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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