受注:045-509-1970 |
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Synonyms | YM 178 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H24N4O2S |
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分子量 | 396.51 | CAS No. | 223673-61-8 | |
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (199.23 mM) | |
Ethanol | 8 mg/mL (20.17 mM) | |||
Water | Insoluble | |||
* <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 | Mirabegron (YM 178) is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM. |
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in vitro | Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively. [1] Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6. [2] |
in vivo | Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction. [1] Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. [3] Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. [4] |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] | PubMed: 32099531 |
Establishment and characterization of a novel cell line, NCC-TGCT1-C1, derived from a patient with tenosynovial giant cell tumor [ Hum Cell, 2020, 10.1007/s13577-020-00425-8] | PubMed: 32886306 |
Establishment and characterization of NCC-MFS2-C1: a novel patient-derived cancer cell line of myxofibrosarcoma [ Hum Cell, 2020, 10.1007/s13577-020-00420-z] | PubMed: 32870449 |
Short-term cold exposure supports human Treg induction in vivo. [ Mol Metab, 2019, 28:73-82] | PubMed: 31427184 |
β3 adrenoceptor-induced cholinergic bladder inhibition involves EPAC1 and PKC favoring ENT1-mediated adenosine outflow from the human and rat detrusor. [ Br J Pharmacol, 2019, 10.1111/bph.14921] | PubMed: 31721163 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。