2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Cannabinoid Receptor Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase TNF Receptor Interleukin Related
  4. GW405833 hydrochloride

GW405833 hydrochloride  (Synonyms: L768242 hydrochloride)

目录号: HY-110036A 纯度: 99.59%
COA 产品使用指南 技术支持

GW405833 (L768242) hydrochloride 是一种有效的、选择性的大麻素受体2 (CB2) 激动剂。GW405833 对 CB2 的 EC50 和 Ki 值为 0.65 nM 和 3.92 nM；对 CB1 的 EC50 和 Ki 值为16.1 μM 和 4772 nM。GW405833 hydrochloride 还表现出非竞争性的 CB1 抑制剂作用，通过依赖于 CB1 受体 (而非 CB2) 的机制发挥镇痛效果。GW405833 hydrochloride 能显著抑制 Forskolin (HY-15371) 刺激产生的 cAMP 的生成。GW405833 hydrochloride 通过下调 HIF-1α 来抑制糖酵解，从而缓解急性肝衰竭 (ALF)。

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GW405833 hydrochloride

GW405833 hydrochloride Chemical Structure

CAS No. : 1202865-22-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1064
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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 GW405833 hydrochloride:

GW405833 hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF)[1][2][3][4][5][6].

IC50 & Target[1][5]

CB2

50.7 nM (IC50)

CB1

16.1 μM (IC50)

IL-1β

 

HIF-1α

 

体外研究
(In Vitro)

GW405833 hydrochloride在人、小鼠和大鼠脾膜中表现为低效激动剂，并在 hCB2-CHO 细胞中表现出反向激动剂作用[4]。
GW405833 (10 μM，25 h) hydrochloride 通过下调 HIF-1α 来抑制糖酵解，从而抑制肝巨噬细胞增殖[5]。

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

GW405833 hydrochloride 相关抗体:

ELISA Assay[5]

Cell Line: RAW264.7 macrophages
Concentration: 10 μM
Incubation Time: After 1 hour of pre-treatment, add LPS for 24 h
Result: Reduced the expressions of TNF-α and IL-1β.

Western Blot Analysis[5]

Cell Line: RAW264.7 macrophages
Concentration: 10 μM
Incubation Time: After 1 hour of pre-treatment, add LPS for 24 h
Result: Inhibited the expression of HIF-1α, PKM2 and CB2R.
体内研究
(In Vivo)

GW405833 (3-30 mg/kg，腹腔注射，单次剂量) hydrochloride 通过 CB1 受体而非 CB2 受体剂量依赖性地逆转小鼠神经性疼痛和炎症性疼痛模型中的机械性异常疼痛，并且不会产生典型的大麻素样作用[1]。
GW405833 (3 mg/kg，静脉注射，单次剂量) hydrochloride 通过减少细胞因子产生和氧化应激来抑制大鼠的炎症和脚部水肿[3]。
GW405833 (10 mg/kg，腹腔注射，单次剂量) hydrochloride 可通过下调 HIF-1α 来抑制糖酵解防止急性肝衰竭 (ALF) 大鼠模型中的细胞死亡[5]。

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

Animal Model: Partial sciatic nerve ligation (PSNL) model to induce neuropathic pain and inflammatory model induced by complete Freund's adjuvant (CFA) (HY-153808) established in CB1KO mice and CB2KO mice, WT mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: 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). Did not produce typical cannabinoid-like effects and did not trigger stage symptoms.
Animal Model: The footpad edema model induced by Carrageenan (HY-125474) model established in Wistar‑albino rats weighing 200-250 g[3]
Dosage: 3 mg/kg
Administration: Intravenous injection (i.v.), single dose
Result: Significantly reduced the levels of serum TNF-α and IL-1β.
Reduced the MDA content in the tissue, increased the GSH level, and inhibited the MPO activity.
Significantly reduced the infiltration of inflammatory cells and restored tissue damage.
Animal Model: ALF model established in male Wistars rats(200-350 g)[5]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly reduced ALT/AST levels, with a downward trend observed in TBIL but not reaching statistical significance.
Reduced F4/80+, significantly inhibited CD86, and increased CD206.
Reduced the expressions of TNF-α and IL-1β, as well as HIF-1α.
The regulatory effects on liver function, inflammatory factors and HIF-1α completely disappeared in CB2R-/- mice.
分子量

483.82

Formula

C23H25Cl3N2O3
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, 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 : 125 mg/mL (258.36 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 2.0669 mL 10.3344 mL 20.6688 mL
5 mM 0.4134 mL 2.0669 mL 4.1338 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

只
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

GW405833 hydrochloride 相关分类

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 2.0669 mL 10.3344 mL 20.6688 mL 51.6721 mL
5 mM 0.4134 mL 2.0669 mL 4.1338 mL 10.3344 mL
10 mM 0.2067 mL 1.0334 mL 2.0669 mL 5.1672 mL
15 mM 0.1378 mL 0.6890 mL 1.3779 mL 3.4448 mL
20 mM 0.1033 mL 0.5167 mL 1.0334 mL 2.5836 mL
25 mM 0.0827 mL 0.4134 mL 0.8268 mL 2.0669 mL
30 mM 0.0689 mL 0.3445 mL 0.6890 mL 1.7224 mL
40 mM 0.0517 mL 0.2584 mL 0.5167 mL 1.2918 mL
50 mM 0.0413 mL 0.2067 mL 0.4134 mL 1.0334 mL
60 mM 0.0344 mL 0.1722 mL 0.3445 mL 0.8612 mL
80 mM 0.0258 mL 0.1292 mL 0.2584 mL 0.6459 mL
100 mM 0.0207 mL 0.1033 mL 0.2067 mL 0.5167 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.

Keywords:

GW4058331202865-22-2L768242GW 405833GW-405833L 768242L-768242Cannabinoid ReceptorEndogenous MetaboliteHIF/HIF Prolyl-HydroxylaseTNF ReceptorInterleukin RelatedHypoxia-inducible factorsHIFsHIF-PHTumor Necrosis Factor ReceptorTNFRILCarrageenanPaw oedemaOxidative stressCannabinoidChronic Constriction injuryNeuropathic painSpinal cordInhibitorinhibitorinhibit

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