1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. YM-58790

YM-58790 是一种有效的 mAChR 拮抗剂。YM-58790 结合 mAChR 亚型的 Ki 值分别为 28 nM (M1 mAChR),260 nM (M2 mAChR),和 15 nM (M3 mAChR)。YM-58790 对大鼠的反射性节律性收缩膀胱加压有较强的抑制活性。

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YM-58790 Chemical Structure

YM-58790 Chemical Structure

CAS No. : 214558-72-2

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Other Forms of YM-58790:

查看 mAChR 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

YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats[1].

IC50 & Target

mAChR3

15 nM (Ki)

mAChR1

28 nM (Ki)

mAChR2

260 nM (Ki)

体外研究
(In Vitro)

YM-58790 (compound 18b) (0-1 μM) shows potent inhibitory effect on urinary bladder contraction, but has little effect on bradycardia. YM-58790 exhibits selective antagonism between urinary bladder contraction and salivary secretion in vitro[1].

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

体内研究
(In Vivo)

YM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice[1].
YM-58790 (6.0 mg/kg; i.v.) shows poor M1 and M2 antagonism effect in vivo on McN-A343-induced pressor in pithed rats, but displays potent efficacy on M3 antagonism with an ED30 value of 0.36 mg/kg (i.v.) and an ID50 value of 2.4 mg/kg (i.v.)[1].
YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats[1].

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

分子量

466.01

Formula

C27H32ClN3O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (214.59 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 2.1459 mL 10.7294 mL 21.4588 mL
5 mM 0.4292 mL 2.1459 mL 4.2918 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 (sealed storage, away from moisture)。-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 (sealed storage, away from moisture)。-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 2.1459 mL 10.7294 mL 21.4588 mL 53.6469 mL
5 mM 0.4292 mL 2.1459 mL 4.2918 mL 10.7294 mL
10 mM 0.2146 mL 1.0729 mL 2.1459 mL 5.3647 mL
15 mM 0.1431 mL 0.7153 mL 1.4306 mL 3.5765 mL
20 mM 0.1073 mL 0.5365 mL 1.0729 mL 2.6823 mL
25 mM 0.0858 mL 0.4292 mL 0.8584 mL 2.1459 mL
30 mM 0.0715 mL 0.3576 mL 0.7153 mL 1.7882 mL
40 mM 0.0536 mL 0.2682 mL 0.5365 mL 1.3412 mL
50 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0729 mL
60 mM 0.0358 mL 0.1788 mL 0.3576 mL 0.8941 mL
80 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6706 mL
100 mM 0.0215 mL 0.1073 mL 0.2146 mL 0.5365 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:
YM-58790
目录号:
HY-101679
需求量: