WP9QY
Based on 1 Customer Validation
WP9QY is an inhibitor targeting TNFα and RANKL, which blocks the TNFα-TNFR1 interaction and inhibits TNFα-mediated apoptosis, cytotoxicity and bone destruction. WP9QY inhibits osteoclastogenesis and promotes osteoblast differentiation, induces chondrocyte proliferation and glycosaminoglycan production, and synergizes with TGF-β3 to promote chondrogenesis. WP9QY effectively repairs full-thickness articular cartilage defects in rabbits via intra-articular injection, and inhibits methylmercury-induced reduction of NeuN-positive cells in mouse brain slices. WP9QY can be applied to the research of diseases related to methylmercury-induced neuronal death, cartilage injury, osteoarthritis and bone loss.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.79%
- No. CAS: 199999-60-5
- Fòrmula: C58H71N11O15S2
- Peso molecular:1226.38
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Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
WP9QY-functionalized PEG hydrogels (100-250 μM; 24 h TNFα exposure, 6 d NGF differentiation culture) protect differentiated PC12 cells from apoptosis induced by 50 ng/mL human TNFα, maintain cell viability, and prevent the elevation of caspase 3/7 activation levels[1].
WP9QY-functionalized PEG hydrogel (100 μM; 24 h) protects encapsulated mouse islets from 50 ng/mL human TNFα-induced apoptosis and impaired insulin secretion, and maintains cell viability and function[1].
WP9QY (10 μM; 72 h) inhibits neuronal cell death induced by 50 μM methylmercury in cultured mouse organotypic brain slices in vitro[2].
WP9QY (100 μM; 14 d) significantly enhances chondrogenic differentiation of hMSCs in a two-dimensional culture system via accumulation of glycosaminoglycan matrix, as confirmed by Alcian Blue staining (HY-D0001) and absorbance measurement[3].
WP9QY (25-100 μM; 72 h) dose-dependently promotes the proliferation of hMSCs cultured in maintenance medium, chondrocyte differentiation medium, and osteoblast differentiation medium, and this result is confirmed by Hoechst 33342 (HY-15559) fluorescence assay[3].
WP9QY (100 μM; 14 d) induces chondrocyte differentiation in both control and RANKL-knockdown C3H10T1/2 cells in a RANKL signaling-independent manner[3].
WP9QY (5-50 μM; 20 min) dose-dependently inhibits RANKL-induced signaling pathways in RAW 264.7 cells, without affecting M-CSF-induced signaling pathways[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:differentiated rat adrenal pheochromocytoma (PC12) cells
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Concentration:100-250 μM WP9QY; 50 ng/mL human TNFα; 50 ng/mL 2.5S NGF
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Incubation Time:24 hours (TNFα exposure); 6 days (NGF differentiation)
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Result:Maintained viability comparable to unchallenged cells in PEG-RGD-WP9QY hydrogels (100 μM and 250 μM WP9QY) under TNFα challenge.
Showed no significant increase in caspase 3/7 activity.
Confirmed minimal cell death via Live/Dead imaging.
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Cell Line:human mesenchymal stem cells (hMSCs)
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Concentration:100 μM
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Incubation Time:14 days
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Result:Increased absorbance at 620 nm to ~0.27, which was significantly higher than control's ~0.17 with p < 0.01.
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Cell Line:mouse chondrogenic ATDC5 cells
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Concentration:25-100 μM
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Incubation Time:18 days
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Result:Induced dose-dependent chondrocytic differentiation, with more intense Alcian Blue staining at 100 μM compared to 25 μM, and no staining in untreated control cells.
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Cell Line:human mesenchymal stem cells (hMSCs)
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Concentration:50-150 μM (with 10 ng/mL TGF-β3 present throughout culture)
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Incubation Time:14 days
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Result:Induced dose-dependent enlargement of hMSC 3D pellets, with larger pellets observed at 150 μM compared to 50 μM.
Increased Alcian Blue-positive cartilage matrix production in treated pellets.
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Cell Line:human mesenchymal stem cells (hMSCs)
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Concentration:100 μM (tested alone and in combination with 20 ng/mL TGF-β3)
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Incubation Time:15 days
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Result:Strongly enhanced chondrogenesis alone, while TGF-β3 alone weakly enhanced chondrogenesis.
Combined treatment resulted in synergistically increased Alcian Blue staining intensity, showing greater chondrogenesis than either treatment alone.
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Cell Line:human mesenchymal stem cells (hMSCs)
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Concentration:100 μM (tested alone and in combination with 10 ng/mL TGF-β3)
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Incubation Time:21 days
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Result:Increased pellet size and induced cartilage matrix production (positive Alcian Blue and Safranin O staining) alone.
TGF-β3 alone increased chondrocytic differentiation but did not affect pellet size.
Combined treatment resulted in synergistically enhanced cartilage matrix production and larger pellet size compared to either treatment alone.
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Cell Line:human mesenchymal stem cells (hMSCs)
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Concentration:25-100 μM
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Incubation Time:72 hours
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Result:Promoted hMSC proliferation in maintenance, chondrocyte-differentiation, and osteoblast-differentiation media in a dose-dependent manner.
Elevated fluorescence intensity at 25 μM compared to untreated controls; further increased intensity at 100 μM, with p < 0.01 for all comparisons to untreated controls.
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Cell Line:mouse mesenchymal C3H10T1/2 cells (control and RANKL-knockdown)
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Concentration:100 μM
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Incubation Time:14 days
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Result:Enhanced chondrocytic differentiation (positive Alcian Blue staining) in both control and RANKL-knockdown C3H10T1/2 cells.
RANKL knockdown had no effect on WP9QY-induced chondrogenesis.
WP9QY (2.1 mg/kg/d; continuous infusion via osmotic minipump; 4 weeks) completely prevents ovariectomy-induced osteoporosis in female C57BL/6J mice, restoring cancellous bone parameters and reducing osteoclast activity to near sham-operated levels[4].
WP9QY (9 mg/kg; s.c.; every 3 hours; 48 hours) completely prevents low dietary calcium2+-induced osteoporosis in male CD-1 mice, restoring cancellous bone parameters and reducing osteoclast activity to near normal-calcium diet levels[4].
WP9QY (4 mg/kg/d; continuous infusion via osmotic minipump; 7 days) completely prevents low dietary calcium2+-induced osteoporosis in both TNFR(I)-/- TNFR(II)-/- and wild-type mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Japanese white (male, 19-20 weeks old)[3]
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Dosage:5 mg
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Administration:intraarticular; 2 doses (days 14 and 21)
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Result:Caused partial filling of articular cartilage defects and expanded Safranin-O-positive regions in defects.
Reduced mean modified Wakitani score to ~7, versus ~12 for vehicle (P=0.04).
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Animal Model:C57BL/6J Mice (female, 12 weeks old, bilateral ovariectomy-induced)[4]
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Dosage:2.1 mg/kg/d
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Administration:continuous infusion via osmotic minipump; 4 weeks
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Result:Maintained bone mineral density of proximal tibiae at levels not significantly different from sham-operated mice.
Restored cancellous bone volume fraction from 9.10% to 14.79%.
Restored trabecular number from 6.10 no./mm to 8.01 no./mm.
Restored trabecular spacing from 150.12 μm to 109.998 μm.
Reduced osteoclast number per bone surface from 7.62 no./mm to 3.65 no./mm.
Reduced osteoclast surface per bone surface from 11.58% to 5.96%.
Blocked the ovariectomy-induced increase in urinary deoxypyridinoline cross-links.
Had no effect on body weight or uterine weight.
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Animal Model:TNFR(I)-/- TNFR(II)-/- Mice (129/B6 background); wild-type (genetically matched, low dietary calcium-induced)[4]
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Dosage:4 mg/kg/d
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Administration:continuous infusion via osmotic minipump; 7 days
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Result:Maintained bone mineral density at levels not significantly different from mice on a normal-calcium diet in both TNFR double-knockout and wild-type mice.
Blocked the low-calcium diet-induced increase in urinary deoxypyridinoline cross-links in both genotypes.
Chemical Information
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No. CAS 199999-60-5
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Appearance Solid
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Peso molecular 1226.38
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Fòrmula C58H71N11O15S2
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Color White to off-white
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Sequence
Tyr-Cys-Trp-Ser-Gln-Tyr-Leu-Cys-Tyr (Disulfide bridge:Cys2-Cys8)
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Sequence Shortening
YCWSQYLCY (Disulfide bridge:Cys2-Cys8)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 100 mg/mL (81.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (0.82 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (299 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lin CC, et al. Functional PEG-peptide hydrogels to modulate local inflammation induced by the pro-inflammatory cytokine TNFalpha. Biomaterials. 2009;30(28):4907-4914. [Content Brief]
[2]. Toyama T, et al. Methylmercury induces neuronal cell death by inducing TNF-α expression through the ASK1/p38 signaling pathway in microglia. Sci Rep. 2021;11(1):9832. Published 2021 May 10. [Content Brief]
[3]. Furuya Y, et al. Induction of chondrogenesis with a RANKL-binding peptide, WP9QY, in vitro and in vivo in a rabbit model. Biochem Biophys Res Commun. 2022;602:98-104. [Content Brief]
[4]. Aoki K, et al. A TNF receptor loop peptide mimic blocks RANK ligand-induced signaling, bone resorption, and bone loss. J Clin Invest. 2006;116(6):1525-1534. [Content Brief]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 | 0.8154 mL | 4.0770 mL | 8.1541 mL | 20.3852 mL |
| 5 mM | 0.1631 mL | 0.8154 mL | 1.6308 mL | 4.0770 mL | |
| 10 mM | 0.0815 mL | 0.4077 mL | 0.8154 mL | 2.0385 mL | |
| 15 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.3590 mL | |
| 20 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0193 mL | |
| 25 mM | 0.0326 mL | 0.1631 mL | 0.3262 mL | 0.8154 mL | |
| 30 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6795 mL | |
| 40 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5096 mL | |
| 50 mM | 0.0163 mL | 0.0815 mL | 0.1631 mL | 0.4077 mL | |
| 60 mM | 0.0136 mL | 0.0680 mL | 0.1359 mL | 0.3398 mL | |
| 80 mM | 0.0102 mL | 0.0510 mL | 0.1019 mL | 0.2548 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
WP9QY Related Classifications
HY-P2612 Related Classifications
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