1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. S-777469

S-777469 是一种选择性,具有口服活性的大麻素 2 型受体 (CB2) 激动剂,Ki 为 36 nM。S-777469 以剂量依赖性方式显著抑制化合物 48/80 诱导的小鼠抓挠行为。S-777469 通过 CB2 兴奋抑制瘙痒信号的传递,从而产生止痒作用。

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S-777469 Chemical Structure

S-777469 Chemical Structure

CAS No. : 885496-53-7

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查看 Cannabinoid 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

S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
> 2000 nM
Compound: 15, S-777469
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins
Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 25 mins
[PMID: 22444677]
CHO IC50
24 nM
Compound: 15, S-777469
Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins
Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release after 45 mins
[PMID: 22444677]
Clinical Trial
分子量

414.47

Formula

C23H27FN2O4

CAS 号
性状

固体

颜色

Off-white to light yellow

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
细胞实验: 

DMSO 中的溶解度 : 83.33 mg/mL (201.05 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 2.4127 mL 12.0636 mL 24.1272 mL
5 mM 0.4825 mL 2.4127 mL 4.8254 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 2.4127 mL 12.0636 mL 24.1272 mL 60.3180 mL
5 mM 0.4825 mL 2.4127 mL 4.8254 mL 12.0636 mL
10 mM 0.2413 mL 1.2064 mL 2.4127 mL 6.0318 mL
15 mM 0.1608 mL 0.8042 mL 1.6085 mL 4.0212 mL
20 mM 0.1206 mL 0.6032 mL 1.2064 mL 3.0159 mL
25 mM 0.0965 mL 0.4825 mL 0.9651 mL 2.4127 mL
30 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0106 mL
40 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5079 mL
50 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2064 mL
60 mM 0.0402 mL 0.2011 mL 0.4021 mL 1.0053 mL
80 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7540 mL
100 mM 0.0241 mL 0.1206 mL 0.2413 mL 0.6032 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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Inquiry Information

产品名称:
S-777469
目录号:
HY-145153
需求量: