製品番号: HY-110036

GW-405833

(別名: L768242)

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Based on 1 Customer Validation

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i 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).

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純度: 98.91%
CAS 番号: 180002-83-9
分子式: C₂₃H₂₄Cl₂N₂O₃
分子量:447.35

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GW-405833 構造式

CAS 番号: 180002-83-9

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]^[5]

CB2

50.7 nM (EC₅₀)

CB1

16.1 μM (EC₅₀)

IL-1β

HIF-1α

Cannabinoid Receptor アイソフォーム固有の製品をすべて表示 :

Endogenous Metabolite アイソフォーム固有の製品をすべて表示 :

HIF/HIF Prolyl-Hydroxylase アイソフォーム固有の製品をすべて表示 :

TNF Receptor アイソフォーム固有の製品をすべて表示 :

Interleukin Related アイソフォーム固有の製品をすべて表示 :

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	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]
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	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]

体外実験

GW-405833 behaves as a low-efficacy agonist in spleen membranes from human, mice and rats and exhibits a reverse agonist effect in hCB2-CHO cells^[4].
GW-405833 (10 μM, 25 h) inhibits the proliferation of hepatic macrophages through downregulating HIF-1α to inhibit glycolysis^[5].

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

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.

体内実験

GW-405833 (3-30 mg/kg, i.p., single dose) dose-dependently reverses mice mechanical abnormal pain in both neuropathic pain and inflammatory pain models through CB1 receptors rather than CB2 receptors and does not produce typical cannabinoid-like effects^[1].
GW-405833 (3 mg/kg, i.v., single dose) inhibits inflammation and footpad edema of rats by reducing cytokine production and oxidative stress^[3].
GW-405833 (10 mg/kg, i.p., single dose) protects against cell death in acute liver failure (ALF) rats model through downregulating HIF-1α to inhibit glycolysis^[5].

MedChemExpress (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.

化学情報

CAS 番号 180002-83-9
性状 Solid
分子量 447.35
分子式 C₂₃H₂₄Cl₂N₂O₃
Color Light yellow to yellow
SMILES

O=C(C1=C(C(Cl)=CC=C1)Cl)N2C3=C(C=C(OC)C=C3)C(CCN4CCOCC4)=C2C
別名

L768242
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 116.67 mg/mL (260.80 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2354 mL

11.1769 mL

22.3539 mL

5 mM

0.4471 mL

2.2354 mL

4.4708 mL

10 mM

0.2235 mL

1.1177 mL

2.2354 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
SDS (420 KB)
- English - EN (420 KB)
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- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Li AL, et al. Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther. 2017 Aug;362(2):296-305. [Content Brief]

[2]. Li J, et al. Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation. Medchemcomm. 2019 Sep 17;10(11):1935-1947. [Content Brief]

[3]. Parlar A, Arslan SO, Doğan MF, et al. The exogenous administration of CB2 specific agonist, GW405833, inhibits inflammation by reducing cytokine production and oxidative stress. Exp Ther Med. 2018;16(6):4900-4908. [Content Brief]

[4]. Marini P, Cascio MG, King A, Pertwee RG, Ross RA. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol. 2013;169(4):887-899. [Content Brief]

[5]. Cai SL, et al. CB2R agonist GW405833 alleviates acute liver failure in mice via inhibiting HIF-1α-mediated reprogramming of glycometabolism and macrophage proliferation. Acta Pharmacol Sin. 2023 Jul;44(7):1391-1403. [Content Brief]

[6]. Valenzano KJ, et al. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48(5):658-72. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

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GW-405833

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Cannabinoid Receptor アイソフォーム固有の製品をすべて表示

Endogenous Metabolite アイソフォーム固有の製品をすべて表示

HIF/HIF Prolyl-Hydroxylase アイソフォーム固有の製品をすべて表示

TNF Receptor アイソフォーム固有の製品をすべて表示

Interleukin Related アイソフォーム固有の製品をすべて表示

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GW-405833 関連分類

HY-110036 関連分類