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TD-5471 hydrochloride

Catalog No.GC31453

TD-5471 hydrochloride is a potent and selective full agonist of the human β2-adrenoceptor.

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TD-5471 hydrochloride Chemical Structure

Cas No.: 530084-35-6

Size Price Stock Qty
1mg
$2,482.00
In stock
5mg
$6,214.00
In stock
10mg
$10,563.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

TD-5471 hydrochloride is a potent and selective full agonist of the human β2-adrenoceptor.

TD-5471 is potent, with slow onset in an in vitro guinea pig trachea model. TD-5471 has potency with pEC50 of 8.7 in the guinea pig tracheal ring assay.TD-5471 is structurally differentiated from Milveterol and its long duration of action is consistent with a correlation with hydrophobicity observed in other long-acting β2-agonist discovery programs[1].

TD-5471 shows a dose-dependent and long duration of action in an in vivo guinea pig model of bronchoprotection. In a guinea pig model of in vivo bronchoprotection, TD-5471 shows excellent potency (measured 1.5 h after nebulized dosing). Because a high dose of Salmeterol (300 μg/mL) provides bronchoprotection lasting ≥24 h in this model, a 72 h time point is selected to provide confidence that TD-5471 will be suitable for once-daily dosing in man. TD-5471-mediated bronchoprotection at 72 h is dose-dependent and is significantly greater than that of Salmeterol at nebulizer concentrations of ≥30 μg/mL[1].

[1]. Jacobsen JR, et al. Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2625-30.

Chemical Properties

Cas No. 530084-35-6 SDF
Canonical SMILES O=C1NC2=C(C([C@@H](O)CNCCC3=CC=C(NC4=CC(C5=CC=CC=C5)=C(OC)C=C4)C=C3)=CC=C2O)C=C1.[H]Cl
Formula C32H32ClN3O4 M.Wt 558.07
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.7919 mL 8.9594 mL 17.9189 mL
5 mM 0.3584 mL 1.7919 mL 3.5838 mL
10 mM 0.1792 mL 0.8959 mL 1.7919 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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