2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. TAK-259 hydrochloride

TAK-259 hydrochloride 是一种具有口服活性的 α1D-肾上腺素能受体 (Adrenergic Receptor) 拮抗剂，对人源 α1D-肾上腺素能受体的 Ki 值为 1.1 nM。TAK-259 hydrochloride 可抑制膀胱出口梗阻模型大鼠离体膀胱条的收缩，减少非排尿性膀胱收缩，改善尿频症状。TAK-259 hydrochloride 可用于膀胱过度活动症的相关研究。

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TAK-259 hydrochloride

TAK-259 hydrochloride Chemical Structure

CAS No. : 1192347-42-4

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Other Forms of TAK-259 hydrochloride:

TAK-259 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TAK-259 hydrochloride is an orally active α1D-adrenergic receptor antagonist with a Ki value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 hydrochloride can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 hydrochloride can be used in research related to overactive bladder[1].

IC50 & Target[1]

Alpha-1D adrenergic receptor

1.1 nM (Ki)

体外研究
(In Vitro)

TAK-259 hydrochloride (Compound 9u) (60 min) 在无细胞膜结合实验中可强效结合人源 α1D-肾上腺素能受体，其 Ki = 1.1 nM[1]。
TAK-259 hydrochloride (10 μM; 5 min at 32°C) 在基于细胞的膜片钳实验中表现出较低的 hERG K+ 通道抑制活性 (10 μM 时抑制率为 16%)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-259 hydrochloride 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Vdss CLtotal Cmax AUC MRT Bioavailability
Rat[1] 0.1 mg/kg i.v. 4432 mL/kg 2395 mL/h/kg / / / /
Rat[1] 1 mg/kg p.o. / / 60.2 ng/mL 358 ng·h/mL 4.53 h 84.5 %
体内研究
(In Vivo)

TAK-259 hydrochloride (静脉注射) 可剂量依赖性地降低膀胱出口梗阻大鼠的非排尿性膀胱收缩，其 IC30 为 12 nM，ID50 为 1.3 µg/kg[1]。
TAK-259 hydrochloride (10 µg/kg；灌胃) 在以最低有效剂量 10 µg/kg 给药时，可降低 Cyclophosphamide (HY-17420) 诱导膀胱炎大鼠的排尿频率[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[1]
Dosage: 10 µg/kg
Administration: p.o.
Result: Increased voiding intervals, representing the minimum effective dose for reducing urinary frequency in this model.
分子量

410.70

Formula

C14H14Cl3N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TAK-259 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAK-2591192347-42-4TAK259TAK 259Adrenergic ReceptorBeta Receptorα1D-adrenergic receptor antagonistoveractive bladderRatsbladder outlet obstruction
Inhibitorinhibitorinhibit

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产品名称：
TAK-259 hydrochloride
目录号：
HY-120473A
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