1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. GW-405833

GW-405833  (Synonyms: L768242)

目录号: HY-110036 纯度: 99.12%
COA 产品使用指南

GW-405833 (L768242) 是一种有效的、选择性的大麻素受体2 (CB2) 激动剂,EC50 值为 50.7 nM。GW-405833 也表现为非竞争性的 CB1 拮抗剂。GW-405833 抑制炎症性和神经性疼痛。

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GW-405833 Chemical Structure

GW-405833 Chemical Structure

CAS No. : 180002-83-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥984
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1 mg ¥400
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5 mg ¥1000
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10 mg ¥1500
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25 mg ¥2700
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50 mg ¥4200
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Other Forms of GW-405833:

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

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain[1][2].

IC50 & Target

CB2

50.7 nM (EC50)

CB1

16.1 μM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
16.1 μM
Compound: GW405833; L768242
Agonist activity at human CB1 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
Agonist activity at human CB1 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
[PMID: 32952995]
CHO EC50
50.7 nM
Compound: GW405833; L768242
Agonist activity at human CB2 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
Agonist activity at human CB2 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
[PMID: 32952995]
体内研究
(In Vivo)

GW-405833 (3, 10 和 30 mg/kg; i.p.) 在 WT 小鼠中以剂量依赖性的方式逆转了两种疼痛模型中的痛觉过敏,而在 CB1KO 小鼠中这种效应被保留,但在 CB2KO 小鼠中这种效应不存在[1]
GW-405833 (30 mg/kg; i.p.) 不引起 CD1KO 小鼠猝倒、运动共济失调、体温过低或急性甩尾抗感觉[1]

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

Animal Model: CB1KO mice, CB2KO mice, WT mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased the paw withdrawal threshold in CB2KO and WT mice in a dose-dependent manner.
Restored mechanical paw withdrawal thresholds relative to baseline in CB2KO and WT mice at doses as low as 10 mg/kg.
Retained antiallodynic effects in CB2KO mice.
Produced a dose-dependent increase in mechanical threshold in WT mice, but this antiallodynic effect was absent in CB1KO mice.
Blocked the antihyperalgesic effect by the CB1 antagonist rimonabant (HY-14136), but not by the CB2 antagonist SR144528 (HY-13439).
分子量

447.35

Formula

C23H24Cl2N2O3

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 116.67 mg/mL (260.80 mM; 超声助溶 (<60°C); 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 2.2354 mL 11.1769 mL 22.3539 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 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。-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

纯度: 99.12%

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。-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 2.2354 mL 11.1769 mL 22.3539 mL 55.8847 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 mL 11.1769 mL
10 mM 0.2235 mL 1.1177 mL 2.2354 mL 5.5885 mL
15 mM 0.1490 mL 0.7451 mL 1.4903 mL 3.7256 mL
20 mM 0.1118 mL 0.5588 mL 1.1177 mL 2.7942 mL
25 mM 0.0894 mL 0.4471 mL 0.8942 mL 2.2354 mL
30 mM 0.0745 mL 0.3726 mL 0.7451 mL 1.8628 mL
40 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3971 mL
50 mM 0.0447 mL 0.2235 mL 0.4471 mL 1.1177 mL
60 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.9314 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6986 mL
100 mM 0.0224 mL 0.1118 mL 0.2235 mL 0.5588 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:
GW-405833
目录号:
HY-110036
需求量: