| Size | Price | Stock | Qty |
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Purity: ≥98%
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)). Male C57BL/6 mice (10–12 weeks old) were used. Pulmonary fibrosis was induced by intratracheal instillation of bleomycin (0.5 mg/kg) or adeno-associated virus AAV6.2m-TGF-β1 (2.5×10¹¹ vg). Olodaterol was administered once daily by inhalation in a whole-body exposure chamber using a jet nebulizer for 5 min. The treatment was either preventive (days 1–20) or therapeutic (days 7–20). On day 21, assessments were performed. [2] Lung density was assessed by micro-computed tomography (μCT) with cardiac gating. Mice were anesthetized, and images were acquired using a μCT system. Hounsfield units were used as a measure of fibrosis. [2] Lung function was measured using a FlexiVent system. Mice were anesthetized, the trachea was cannulated, and they were ventilated with a tidal volume of 10 mL/kg and an end-expiratory pressure of 3 cmH₂O. Parameters including forced vital capacity (FVC) were analyzed. [2] After lung function measurement, bronchoalveolar lavage was performed twice with 0.8 mL lavage buffer. Total and differential cell counts were determined. Lungs were weighed, and right lungs were frozen for analysis; left lungs were fixed with 4% paraformaldehyde for histology. [2] Ashcroft scoring was performed on Masson’s trichrome-stained lung sections using a microscope with a 10× objective, with samples blinded prior to scoring. [2] Protein levels in BALF and lung homogenates were measured using ELISA kits for TGF-β, MMP-9, TIMP-1, and pro-inflammatory panels. Total protein was quantified using a BCA assay. [2] RNA was extracted from lung tissues using phenol-chloroform and column-based kits. qRT-PCR was performed using TaqMan assays for Col1A1, Col3A1, and the housekeeping gene PolA2. [2] |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Drug Use During Lactation While there is currently no published data on the use of olodaterol during lactation, data on the related drug terbutaline suggest that very small amounts are expected to be excreted into breast milk. The authors of several reviews agree that the use of such drugs during lactation is acceptable due to the low bioavailability of inhaled bronchodilators and the low maternal serum concentrations after administration. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. |
| References |
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| Additional Infomation |
Olodaterol hydrochloride is a hydrochloride salt composed of olodaterol and an equivalent amount of hydrochloric acid. It is used for the long-term treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (including chronic bronchitis and/or emphysema). It is a beta-adrenergic agonist and bronchodilator. It contains olodaterol (1+).
See also: Olodaterol (with active fraction); Olodaterol hydrochloride; Tiotropium bromide (ingredient)... See more... Drug Indications Treatment of cystic fibrosis |
| Molecular Formula |
C21H27CLN2O5
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|---|---|
| Molecular Weight |
422.906
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| Exact Mass |
422.161
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| Elemental Analysis |
C, 59.64; H, 6.44; Cl, 8.38; N, 6.62; O, 18.92
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| CAS # |
869477-96-3
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| Related CAS # |
Olodaterol;868049-49-4
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| PubChem CID |
11711522
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| Appearance |
White to light yellow solid powder
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| LogP |
3.654
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
521
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[C@H](C1C=C(O)C=C2NC(COC=12)=O)(O)CNC(C)(C)CC1C=CC(OC)=CC=1.Cl
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| InChi Key |
KCEHVJZZIGJAAW-FERBBOLQSA-N
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| InChi Code |
InChI=1S/C21H26N2O5.ClH/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);1H/t18-;/m0./s1
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| Chemical Name |
6-hydroxy-8-[(1R)-1-hydroxy-2-[[1-(4-methoxyphenyl)-2-methylpropan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one;hydrochloride
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| Synonyms |
Olodaterol hydrochloride BI 1744 BI1744BI-1744 Olodaterol StriverdiOlodaterol HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02682862 | COMPLETED | Drug: olodaterol hydrochloride 2.5mcg, tiotropium bromide 2.5mcg Drug: olodaterol 2.5 mcg |
Asthma | University of Dundee | 2016-07-11 | Phase 4 |
| NCT02799784 | COMPLETEDWITH RESULTS | Drug: UMEC/VI Drug: TIO/OLO Drug: Albuterol/salbutamol |
Pulmonary Disease, Chronic Obstructive | GlaxoSmithKline | 2016-07-14 | Phase 4< |
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