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Synonyms | SL 75212 HCl | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H29NO3.HCl |
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分子量 | 343.89 | CAS No. | 63659-19-8 | ||||
Solubility (25°C)* | 体外 | DMSO | 69 mg/mL (200.64 mM) | ||||
Water | 69 mg/mL (200.64 mM) | ||||||
Ethanol | 69 mg/mL (200.64 mM) | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM. |
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in vitro | Betaxolol is able to protect retinal neurones. [2] Betaxolol attenuates the NMDA-induced influx of 45Ca2+ while β-adrenoreceptor agonists are ineffective. [3] The glutamate-induced release of LDH is almost completely prevented when betaxolol (10 μM) is included. [4] Betaxolol (100 μM) is very effective in preventing the hypoxia-induced release of LDH from cortical cultures. [5] |
in vivo | When Betaxolol is injected i.p. into the rats before ischaemia and on the days of reperfusion the changes to the calretinin and ChAT immunoreactivities are reduced and the reduction of the b-wave is prevented. Inclusion of betaxolol partially prevents the changes caused by NMDA and lack of oxygen/glucose. [5] |
細胞アッセイ | 細胞株 | Dissociated rat cortical cells |
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濃度 | 100 μM | |
反応時間 | 4 hours | |
実験の流れ | Dissociated cortical cells from 16–18-day-old fetal rats are grown, in 35 mm dishes, in DMEM supplemented with L-glutamine (4 mM), glucose (6 g/L), penicillin (100 U/mL), streptomycin (100 μg/mL) and 10% hormonal supplemented medium consisting of transferrin (1 mg/mL), insulin (250 μg/mL) putrescine (600 μM), sodium selenite (0.3 μM), progesterone (0.2 μM) and estradiol (0.1 pM) for 7 days in an atmosphere of 5% CO2/95% O2 at 37 °C. The cultures are then transferred to a culture medium which lacks the hormonal supplemented medium. L-glutamate is added to the medium and incubated for a further 4 hours under normoxic conditions. Betaxolol are added to the cultures at the same time as L-glutamate. In other experiments the cultures are subjected to anoxic conditions, 95% N2/5% CO2, for 5 hours at 37 °C. Betaxolol is added prior to anoxia. Reoxygenation is then achieved by replacing the cells in normoxic conditions (95% O2/5% CO2) for 3 hours. Cellular injury is assessed by measuring lactate dehydrogenase (LDH) release into the cell culture supernatant after hypoxia/reoxygenation or glutamate exposure. LDH activity is assayed spectrophotometrically by following NADH metabolism for 2 minutes at 340 nm. | |
動物実験 | 動物モデル | Rat wiht ischaemia |
投薬量 | 2.5 mg/kg | |
投与方法 | Administered via i.p. |
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Box-Behnken response surface modeling assisted enantiomeric resolution of some racemic β-blockers using HPTLC and β-cyclodextrin as chiral mobile phase additive: Application to check the enantiomeric purity of betaxolol [ Chirality, 2018, 30(11):1195-1205] | PubMed: 30193408 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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