Salmeterol Xinafoate

SKU: orb1300582

Description

Research Area

Infectious Disease & Virology, Neuroscience, Pharmacology & Drug Discovery, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	94749-08-3
MW	603.75
Purity	98.00%
Formula	C₃₆H₄₅NO₇
SMILES	OCc1cc(ccc1O)C(O)CNCCCCCCOCCCCc2ccccc2.O=C(O)c2ccc1ccccc1c2O
Target	HIV Protease,Adrenergic Receptor
Solubility	Ethanol:12.1 mg/mL (20.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.31 mM);DMSO:60.4 mg/mL (100.04 mM)

Bioactivity

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Target IC50	β2-adrenoceptor:9.6 (pEC50)\|β2-adrenoceptor (WT):1.5 nM (Ki)\|β3-adrenoceptor:5.9 (pEC50)\|β1-adrenoceptor:6.1 (pEC50)
In Vivo	The OVA/LPS groups with salmeterol result in a significant decrease in the enhanced AHR in allergic mice in a dose-dependent manner. Salmeterol contends with asthma via regulating the inflammation of the airway of the mice. Read more...
In Vitro	Salmeterol significantly inhibits production of pro-inflammatory mediators by RAW264.7 and THP-1 cells. Salmeterol downregulates PgLPS-mediated phosphorylation of the ERK1/2 and JNK but not p38 MAP kinases (MAP-K). Salmeterol also attenuates the activation of NF-κB via inhibition of nuclear translocation of p65-NFκB, the transcriptional activity of NF-κB and IκBα phosphorylation. Salmeterol shows very high selectivity for the WT β2AR (β1 Ki /β2 Ki ratio of approximately 1500) with Ki of 1.5±0.4 nM. Salmeterol prevents phosphorylation levels of IRS-1Ser307 induced by tumor necrosis factor-α. Salmeterol alone prevents cell death in retinal Müller cells (p<0.05 versus 25 mM glucose). Salmeterol in conbination with IRS-1 shRNA shows a significant increase in cell death compared to salmeterol alone. Moreover, salmeterol alone treatment significantly reduces cytochrome C levels, with the effect lessened when salmeterol is combined with IRS-1 shRNA. Salmeterol (100 μM) causes apoptosis of DCs, and can not affect the differentiation and maturation of DCs at 10 μM. Salmeterol (10 μM) decreases the mRNA and protein levels of pro-inflammatory cytokines in LPS-activated DCs and inhibits MAPK and NF-κB activation Read more...
Animal Research	Salmeterol is formulated in PBS.All mice are sensitized on days 0 and 14 by intraperitoneal injection of either PBS or 0.08 mg OVA and 0.1 mL aluminum hydroxide in 0.1 mL of PBS (pH 7.4). After sensitization, animals are exposed to aerosolized PBS-only (negative control), 1% OVS/PBS (acute exposure), 1% OVA/0.01% LPS/PBS (extra LPS exposure) or 1% OVA/0.01% LPS/salmeterol/PBS (sal treatment) for 40 min, once per day for 3 consecutive days (days 24-26). On day 27, the mice are killed and lungs are divided into two groups for analysis: the left lung lobes are lavaged three times with 1 mL of PBS with 1% fetal calf serum and 5 U/mL heparin, and the right halves are fixed by 4% paraformaldehyde for histological analysis. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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corticosteroid, combination, Beta Receptor, agonist, Adrenergic Receptor, AdrenergicReceptor, Arial, inflammatory, inhibit, GR 33343X, GR 33343X xinafoate, HIVProtease, HIV Protease, Inhibitor, Salmetedur, Salmeterol, Salmeterol Xinafoate, WT β2AR, therapy, β2-adrenergic receptor

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Compound Identifiers

PubChem CID

56801 ↗

Key Properties

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No computed properties available.

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