Art. -Nr.: HY-N11080

Cucurbitacin R

Name: Cucurbitacin R
Brand: MedChemExpress
SKU: HY-N11080
Price: 963.00 USD
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Cucurbitacin R is an orally active anti-inflammatory agent. Cucurbitacin R is isolated from the roots of Cayaponia tayuya. Cucurbitacin R inhibits Cyclooxygenase-2. Cucurbitacin R inhibits Interleukin-6-induced STAT3 activation and cytokine production, blocks NF-κB activation, and selectively prevents NFAT nuclear translocation without affecting Calcineurin activity. Cucurbitacin R inhibits TNF-α production and Nitric-oxide synthase-2 expression. Cucurbitacin R reduces joint damage, soft tissue swelling, paw edema, ear edema, inflammatory cell infiltration, and epithelial thickness. Cucurbitacin R can be used for research on arthritis and delayed-type hypersensitivity.

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Reinheit : 97.56%
CAS. Nr.: 55903-92-9
Formel: C₃₀H₄₆O₇
Molecular Weight:518.68

Speicherung:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Cucurbitacin R Chemical Structure

CAS. Nr.: 55903-92-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

COX-2

STAT3

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Alle NF-κB Isoform-spezifische Produkte anzeigen :

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Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC50	65 μM	Inhibition of TNF-α production in lipopolysaccharide-stimulated RAW 264.7 murine macrophages incubated for 24 hrs by enzyme immunoassay. Inhibition of TNF-α production in lipopolysaccharide-stimulated RAW 264.7 murine macrophages incubated for 24 hrs by enzyme immunoassay.	17065367

In Vitro

Innate ImmunityCytokines & ChemokinesCytokines and ChemokinesCell Cycle Regulation

Innate Immunity

Cytokines & Chemokines

Cucurbitacin R (25-100 μM; 24 h) inhibits nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 mouse macrophages^[1].
Cucurbitacin R (100 μM; 24 h) inhibits prostaglandin E₂ production in lipopolysaccharide-stimulated RAW 264.7 mouse macrophages^[1].
Cucurbitacin R (25-100 μM; 2 h) does not directly affect Nitric-oxide synthase-2 activity in lipopolysaccharide-stimulated RAW 264.7 mouse macrophages^[1].
Cucurbitacin R (25-100 μM; 2 h) directly inhibits cyclooxygenase-2 activity in lipopolysaccharide-stimulated RAW 264.7 mouse macrophages^[1].

Innate Immunity

Cytokines and Chemokines

Cucurbitacin R (6.25-100 μM; 1 h) inhibits TNF-α production in lipopolysaccharide-stimulated RAW 264.7 mouse macrophages^[1].
Cucurbitacin R (30 μM; 18 h) inhibits the production of IL-2, IL-4, IL-10, and interferon-γ and decreases their mRNA expression in Phytohemagglutinin A-stimulated T lymphocytes^[2].

Cell Cycle Regulation

Cucurbitacin R (10-30 μM; 96 h) inhibits phytohemagglutinin A-stimulated T lymphocyte proliferation with an IC₅₀ of 18 μM and induces cell cycle arrest at the G₀ phase^[2].

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

ELISA Assay^[1]

Cell Line:

RAW 264.7 murine macrophages
Concentration:

100 μM
Incubation Time:

24 h
Result:

Inhibited prostaglandin E₂ production by 53%.

ELISA Assay^[1]

Cell Line:

RAW 264.7 murine macrophages
Concentration:

100, 50, 25, 12.5, 6.25 μM
Incubation Time:

1 h
Result:

Inhibited TNF-α production in a concentration-dependent manner with an IC₅₀ value of 65 μM.

ELISA Assay^[2]

Cell Line:

Human T lymphocytes
Concentration:

30 μM (RT-PCR); various concentrations (ELISA)
Incubation Time:

18 h (RT-PCR); 4 days (ELISA)
Result:

Inhibited the production of IL-2, IL-4, IL-10, and interferon-γ by stimulated T lymphocytes.
Reduced cytokine mRNA expression with respect to the control group.

In Vivo

Innate ImmunityCytokines and ChemokinesCytokines & ChemokinesOthers

Innate Immunity

Cytokines and Chemokines

Cucurbitacin R (1-0.25 mg/kg; p.o.; once daily; days 17 to 23) reduces inflammation and bone damage in Lewis rat adjuvant arthritis, decreasing hind paw swelling by 48% at 1 mg/kg p.o. and lowering TNF-α, prostaglandin E₂, and nitric-oxide synthase-2 levels^[1].

Cytokines & Chemokines

Cucurbitacin R (10 mg/kg; i.p.; 0 h and 16 h after challenge) significantly inhibits SRBC-induced DTH edema in mice at 10 mg/kg (i.p.) with an inhibition rate of 61-64%, and reduces TNF-α, IL-1β, and IL-4 levels in inflammatory tissues^[2].

Innate Immunity

Cucurbitacin R (4 mg/kg; p.o.; single administration; 1 h before carrageenan injection) exhibits weak anti-inflammatory activity in the Carrageenan (HY-125474)-induced mouse paw edema model, with an inhibition rate of 27% at 5 h^[3].
Cucurbitacin R (3 mg/kg; i.p.; single dose; 30 min before PLA₂ injection) exhibits anti-inflammatory activity in the PLA₂-induced mouse paw edema model, with an inhibition rate of 61% at 60 min^[3].
Cucurbitacin R (0.5 mg/kg; subcutaneous injection; single dose; 3 h before serotonin injection) exhibits anti-inflammatory activity in the Serotonin (HY-B1473A)-induced mouse paw edema model with an inhibition rate of 79%, and its effect depends on protein synthesis but not on the glucocorticoid receptor^[3].
Cucurbitacin R (0.1 mg/ear, 4 mg/kg; topical, p.o.; administered simultaneously with TPA, single dose) exhibits potent anti-inflammatory activity in the TPA-induced acute mouse ear edema model, with an inhibition rate of 87% at 0.1 mg/ear topically and 36% at 4 mg/kg p.o.^[3].

Others

Cucurbitacin R (10 mg/kg; p.o.) shows analgesic activity in the mouse acetic acid writhing test, with a 47% reduction in writhing responses^[1].
Cucurbitacin R (0.1-0.5 mg/ear; topical administration; 2, 24, and 48 h after challenge) inhibits oxazolone-induced DTH responses in mice, with a maximum inhibition rate of 60% at 0.5 mg/ear, whereas the 0.1 mg/ear dose is ineffective^[2].
Cucurbitacin R (0.1-0.5 mg/ear; topical administration; 2, 24, and 48 h after challenge) inhibits DNFB-induced DTH responses in mice, with a maximum inhibition rate of 40% at 0.5 mg/ear, whereas the 0.1 mg/ear dose is ineffective^[2].
Cucurbitacin R (5 mg/kg; p.o.; single dose; 1 h before acetic acid injection) shows no analgesic activity in the acetic acid writhing test^[3].

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

Animal Model:

Lewis rats (female, 7 weeks old, 200-240 g)^[1]
Dosage:

1 mg/kg (paw swelling); 0.25 mg/kg (paw swelling)
Administration:

p.o.; once daily; days 17 to 23
Result:

Reduced hind paw swelling by 48% at 1 mg/kg.
Reduced hind paw swelling by 10% at 0.25 mg/kg.
Inhibited in vivo production of prostaglandin E2 by 94%.
Inhibited TNF-α production in arthritic paws by 76%.
Reduced nitric-oxide synthase-2 and cyclooxygenase-2 expression in paw homogenates.

Animal Model:

Swiss mice (female, 8 weeks old, 25-30 g)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; 1 h before acetic acid injection
Result:

Showed significant analgesic activity with a 47% reduction in writhing compared with the control group.

Animal Model:

Swiss mice (female, 8 weeks old, 25-30 g)^[2]
Dosage:

0.1, 0.3, 0.5 mg/ear
Administration:

topical; 2, 24, and 48 h after challenge
Result:

At 0.1 mg/ear, had no effect.
At 0.3 mg/ear, reduced ear edema with inhibition percentages of 45% at 24 h, 49% at 48 h, and 39% at 72 h.
At 0.5 mg/ear, reduced ear edema with inhibition percentages of 50% at 24 h, 60% at 48 h, and 53% at 72 h.\nAt 0.1 mg/ear, had no effect.
At 0.3 mg/ear, reduced ear edema with inhibition percentages of 23% at 24 h, 35% at 48 h, and 27% at 72 h.
At 0.5 mg/ear, reduced ear edema with inhibition percentages of 30% at 24 h, 40% at 48 h, and 40% at 72 h.

Animal Model:

Swiss mice (female, 8 weeks old, 25-30 g)^[2]
Dosage:

10 mg/kg
Administration:

i.p.; 0 h and 16 h after challenge
Result:

At 10 mg/kg, significantly reduced paw edema with inhibition percentages of 64% at 18 h, 61% at 24 h, and 62% at 48 h.
Reduced cytokine levels in inflamed paws: TNF-α was 244 pg/mL, IL-1β was 542 pg/mL, and IL-4 was 9 pg/mL.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

4 mg/kg
Administration:

p.o.; single dose; 1 h before carrageenan injection
Result:

Inhibited paw oedema by 27% at 5 h.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

3 mg/kg
Administration:

i.p.; single dose; 30 min before PLA₂ injection
Result:

Inhibited the oedema by 61% at 60 min.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

0.5 mg/kg
Administration:

s.c.; single dose; 3 h before serotonin injection
Result:

Inhibited serotonin-induced paw oedema by 79%.
The anti-oedema effect was not modified by mifepristone, but was abolished by cycloheximide.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

0.1 mg/ear (topical); 4 mg/kg (p.o.)
Administration:

topical (simultaneous with TPA); p.o. (single dose)
Result:

Inhibited the oedema by 87% when administered topically at 0.1 mg/ear.
Showed 36% inhibition when administered orally at 4 mg/kg.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

0.1-0.2 mg/ear
Administration:

topical; twice daily for four days (morning only on the last day)
Result:

At 0.1 mg/ear, inhibited swelling by 56% and neutrophil infiltration by 69%.
At 0.2 mg/ear, inhibited swelling by 60% and neutrophil infiltration by 75%.
Reduced epithelium thickness to 6.37 cells compared to 7.43 in the control.

Animal Model:

Swiss mice (female, 25-30 g)^[3]
Dosage:

5 mg/kg
Administration:

p.o.; single dose; 1 h before acetic acid injection
Result:

Showed no significant analgesic properties at the dose assayed.

Related Protocols :

Chemical Information

CAS. Nr. 55903-92-9
Appearance Solid
Molecular Weight 518.68
Formel C₃₀H₄₆O₇
Color White to off-white
SMILES

C[C@]12[C@@]([C@@]([C@@H](C1)O)([H])[C@@](C)(O)C(CCC(C)(O)C)=O)(CC([C@@]3([C@@]2([H])CC=C4[C@@]3([H])C[C@@H](C(C4(C)C)=O)O)C)=O)C
Structure Classification
- Terpenoids
- Triterpenes
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (19.28 mM; Need ultrasonic and warming; 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

1.9280 mL

9.6399 mL

19.2797 mL

5 mM

0.3856 mL

1.9280 mL

3.8559 mL

10 mM

0.1928 mL

0.9640 mL

1.9280 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (308 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[1]. Escandell JM, et al. Cucurbitacin R reduces the inflammation and bone damage associated with adjuvant arthritis in lewis rats by suppression of tumor necrosis factor-alpha in T lymphocytes and macrophages. The Journal of pharmacology and experimental therapeutics. 2007 Feb;320(2):581-90.

[2]. Escandell JM, et al. Inhibition of delayed-type hypersensitivity by Cucurbitacin R through the curbing of lymphocyte proliferation and cytokine expression by means of nuclear factor AT translocation to the nucleus. The Journal of pharmacology and experimental therapeutics. 2010 Feb;332(2):352-63.

[3]. Recio MC, et al. Anti-inflammatory activity of two cucurbitacins isolated from Cayaponia tayuya roots. Planta medica. 2004 May;70(5):414-20. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9280 mL	9.6399 mL	19.2797 mL	48.1993 mL
	5 mM	0.3856 mL	1.9280 mL	3.8559 mL	9.6399 mL
	10 mM	0.1928 mL	0.9640 mL	1.9280 mL	4.8199 mL
	15 mM	0.1285 mL	0.6427 mL	1.2853 mL	3.2133 mL

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Cucurbitacin R

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