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. GW-405833

GW-405833  (Synonyms: L768242)

目录号: HY-110036 纯度: 98.91%
COA 产品使用指南 技术支持

GW-405833 (L768242) 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。GW-405833 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) 的机制发挥镇痛和消炎效果。GW-405833 能显著抑制 Forskolin (HY-15371) 刺激产生的 cAMP 的生成。GW405833 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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GW-405833

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
In-stock
1 mg ￥400
In-stock
5 mg ￥1000
In-stock
10 mg ￥1500
In-stock
25 mg ￥2700
In-stock
50 mg ￥4200
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Customer Review

Other Forms of GW-405833:

GW-405833 相关抗体

Top Publications Citing Use of Products

查看 Cannabinoid Receptor 亚型特异性产品:

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CB1 CB2

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HIF-1α HIF

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 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. 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. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF)[1][2][3][4][5].

IC50 & Target[1][5]

CB2

50.7 nM (EC50)

CB1

16.1 μM (EC50)

IL-1β

 

HIF-1α

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.65 nM
Compound: 2, GW-405833
Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level
[PMID: 18255291]
CHO EC50
16.1 x 103 nM
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]
体外研究
(In Vitro)

GW-405833 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]。
GW-405833 (10 μM，25 h) 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.

GW-405833 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)

GW-405833 (3-30 mg/kg，腹腔注射，单次剂量) 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]。
GW-405833 (3 mg/kg，静脉注射，单次剂量) 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]。
GW-405833 (10 mg/kg，腹腔注射，单次剂量) 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: 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). 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: Increased the survival rate of mice.
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

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

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

纯度: 98.91%

COA (287 KB) HNMR (263 KB) LCMS (96 KB)

产品使用指南 (1538 KB)
参考文献

GW-405833 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。-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.

Keywords:

GW-405833180002-83-9L768242GW405833GW 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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