1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Upidosin

Upidosin  (Synonyms: Rec 15/2739; Recordati 15/2739; SB 216469)

目录号: HY-106954 纯度: 99.58%
COA 产品使用指南

Upidosin (Rec 15/2739) 是 α-1 肾上腺素受体 (α-1 AR) 拮抗剂。Upidosin 具有对 α-1A AR 亚型的中等选择性。Upidosin 具有尿选择性,在尿道和前列腺有更高的亲和力,Kb 值为 2-3 nM,在耳动脉和主动脉的 Kb 值为 20-100 nM。Upidosin 抑制 [3H]prazosin 与人 α-1A 肾上腺素受体结合。Upidosin 可用于尿道梗阻的研究。

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Upidosin Chemical Structure

Upidosin Chemical Structure

CAS No. : 152735-23-4

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查看 Adrenergic Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction[1].

体外研究
(In Vitro)

Upidosin is one of the most potent compounds action on the prostate with comparing the apparent pKB values, but its potency is slightly lower than that of tamsulosin and is higher than the potencies of prazosin, terazosin and 5-methylurapidil[2].
Upidosin shows binding affinities to cloned humanα1A, humanα1B, humanα1D adrenoceptors with pKi value of 9.0, 7.5 and 8.6, respectively[3].

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

体内研究
(In Vivo)

Upidosin shows greater selectivity than any other α-1 AR antagonist terazosin and tamsulosin in the anesthetized dog[1].
Upidosin (1-300 μg/kg; i.v.) is a more potent antagonist of phenylephrine mediated increases in prostatic pressure with a pA2 value of 8.74 compared to blood pressure with a pA2 value of 7.51[3].

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

分子量

511.61

Formula

C31H33N3O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (488.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9546 mL 9.7731 mL 19.5461 mL
5 mM 0.3909 mL 1.9546 mL 3.9092 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9546 mL 9.7731 mL 19.5461 mL 48.8653 mL
5 mM 0.3909 mL 1.9546 mL 3.9092 mL 9.7731 mL
10 mM 0.1955 mL 0.9773 mL 1.9546 mL 4.8865 mL
15 mM 0.1303 mL 0.6515 mL 1.3031 mL 3.2577 mL
20 mM 0.0977 mL 0.4887 mL 0.9773 mL 2.4433 mL
25 mM 0.0782 mL 0.3909 mL 0.7818 mL 1.9546 mL
30 mM 0.0652 mL 0.3258 mL 0.6515 mL 1.6288 mL
40 mM 0.0489 mL 0.2443 mL 0.4887 mL 1.2216 mL
50 mM 0.0391 mL 0.1955 mL 0.3909 mL 0.9773 mL
60 mM 0.0326 mL 0.1629 mL 0.3258 mL 0.8144 mL
80 mM 0.0244 mL 0.1222 mL 0.2443 mL 0.6108 mL
100 mM 0.0195 mL 0.0977 mL 0.1955 mL 0.4887 mL
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.

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产品名称:
Upidosin
目录号:
HY-106954
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