SML2480
米拉贝隆
≥98% (HPLC), β3-adrenoceptor agonist, powder
别名:
2-氨基-N-[4-[2-[[(2R)-2-羟基-2-苯乙基]氨基]乙基]苯基]-4-噻唑乙酰胺, 2-（2-氨基-1,3-噻唑-4-基）-N-[4-[2-[（（2R）-2-羟基-2-苯乙基）氨基]乙基]苯基]乙酰胺, YM 178, YM178(R)-米拉贝隆
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关于此项目
经验公式（希尔记法）:
C21H24N4O2S
化学文摘社编号:
分子量:
396.51
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
产品名称
米拉贝隆, ≥98% (HPLC)
InChI
1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1
SMILES string
O[C@@H](CNCCC1=CC=C(NC(CC2=CSC(N)=N2)=O)C=C1)C3=CC=CC=C3
InChI key
PBAPPPCECJKMCM-IBGZPJMESA-N
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -16 to -22°, c = 0.5 in methanol
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
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Application
米拉贝隆（Mirabegron）已被用作体外实验中的β3-肾上腺素能受体（β3-AR） 激动剂，用于确定β3-AR 刺激是否特异性地激活人棕色脂肪组织（BAT）生热。
Biochem/physiol Actions
强效和选择性β3-肾上腺素受体激动剂
米拉贝隆是一种强效、选择性β3-肾上腺素能受体激动剂，可激活膀胱逼尿肌中的β3-肾上腺素能受体，导致肌肉松弛和膀胱容量增加。
米拉贝隆是一种非抗毒蕈碱口服活性药，有望用于治疗具有膀胱过度活动症（OAB）症状的患者。它以β3-AR为靶点对尿频储存期的神经控制起作用，从而有助于膀胱的放松。 米拉贝隆也用于治疗儿科患者的神经源性逼尿肌过度活动（NDO）。
signalword
Warning
hcodes
Hazard Classifications
Repr. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Toshiyuki Takasu et al.
The Journal of pharmacology and experimental therapeutics, 321(2), 642-647 (2007-02-13)
We evaluated the pharmacological characteristics of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]-ethyl} acetanilide (YM178). YM178 increased cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human beta3-adrenoceptor (AR). The half-maximal effective concentration (EC50) value was 22.4 nM. EC50 values of YM178 for human beta1-
Kentaro Konishi et al.
European journal of drug metabolism and pharmacokinetics, 43(3), 301-309 (2017-11-23)
Mirabegron is cleared by multiple mechanisms, including drug-metabolizing enzymes. One of the most important clearance pathways is direct glucuronidation. In humans, M11 (O-glucuronide), M13 (carbamoyl-glucuronide), and M14 (N-glucuronide) have been identified, of which M11 is one of the major metabolites
Susan J Keam
Paediatric drugs, 23(4), 411-415 (2021-06-01)
Mirabegron (MYRBETRIQ®), a beta-3 adrenergic agonist developed by Astellas Pharma Inc., is well established as a treatment for overactive bladder in adults and is available as extended-release (ER) tablets administered once daily. More recently, mirabegron has been investigated in pediatric
Rebecca Bragg et al.
The Consultant pharmacist : the journal of the American Society of Consultant Pharmacists, 29(12), 823-837 (2014-12-19)
To review the literature regarding the efficacy and safety of mirabegron for the treatment of overactive bladder (OAB). A literature search was performed using MEDLINE (PubMed) prior to December 31, 2013, using the terms "mirabegron" and "randomized-controlled trial." All published
Pradeep Tyagi et al.
Expert opinion on drug safety, 10(2), 287-294 (2010-12-15)
Mirabegron is being developed as a new treatment for the management of overactive bladder (OAB). It is an orally active drug that works by activating the β(3)-adrenoceptor with a better safety profile than antimuscarinic drugs. However, long-term adverse effects are
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