ZY39
Based on 1 Customer Validation
ZY39 is a SaClpP agonist. ZY39 promotes the enzymatic hydrolysis of SaClpP and HsClpP in vitro. ZY39 inhibits the growth of Staphylococcus aureus strains. ZY39 reduces the load of Staphylococcus aureus in organs and ascites in mouse peritonitis models and zebrafish infection models, and improves the survival rate of model animals. ZY39 can be used in studies related to Staphylococcus aureus infection, such as peritonitis.
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- Purity: 99.73%
- CAS No.: 2999673-51-5
- 화학식: C28H35F3N4O4
- 분자량:548.60
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보관:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
ZY39 potently activates SaClpP-mediated α-casein hydrolysis in vitro with an EC50 of 1.1 μM, and exhibits agonistic activity during the hydrolysis of fluorescein isothiocyanate-casein (FITC-casein) by S. aureus ClpP protease (SaClpP), with an EC50 of 0.33 μM[1].
ZY39 activates the hydrolysis of α-casein by HsClpP in vitro with an EC50 of 3.6 μM, but exhibits extremely low activity against gut microbial ClpP (EcClpP, LaClpP)[1].
ZY39 potently inhibits the growth of both drug-sensitive and multidrug-resistant S. aureus strains in vitro. Its activity depends on functional SaClpP, with MIC values ranging from 0.031 to 0.13 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ZY39 (25-50 mg/kg; i.p.; single dose) achieves 89-100% survival and reduces bacterial loads by 2-4 log CFU/g tissue in mice with S. aureus USA300-induced peritonitis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zebrafish (7 to 11 months old, 300 mg, regardless of gender)[1]
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Dosage:0.5 mg/kg; 5 mg/kg; 25 mg/kg
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Administration:i.p.; single dose
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Result:Showed therapeutic effects comparable to (R)-ZG197 (HY-152096) at 25 mg/kg in zebrafish infected with a lethal inoculum of USA300 that killed all control zebrafish within 24 hours (5 mg/kg dose).
Provided significantly improved rescue rates compared to Vancomycin (HY-B0671) at the same dose in zebrafish infected with a USA300 inoculum that killed 80% of control zebrafish within 48 h (0.5 mg/kg dose).
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Animal Model:ICR (CD1) mice (female, 20-22 g)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.p.; single dose
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Result:Resulted in 89-100% survival rates, comparable to vancomycin at 25 mg/kg (25 mg/kg and 50 mg/kg doses).
Reduced bacterial loads by 2-4 log CFU/g tissue in heart, liver, spleen, lung, kidney, and peritoneal fluid compared to vehicle controls (25 mg/kg and 50 mg/kg doses).
Provided 100% survival in S. aureus MRSA XJ049-infected mice, compared to 56% survival with oxacillin at 50 mg/kg.
Chemical Information
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CAS No. 2999673-51-5
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Appearance Solid
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분자량 548.60
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화학식 C28H35F3N4O4
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Color White to off-white
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SMILES
FC(F)(F)CCCNC(N1[C@]2([H])N(C(CC1)=O)[C@@](C(N(C2)CC3=CC=C(OC)C4=C3C=CC=C4)=O)([H])[C@@H](C)CC)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
DMSO : 100 mg/mL (182.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.56 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (protect from light, stored under nitrogen)
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.
순도&문서
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
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 (protect from light, stored under nitrogen). 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 | 1.8228 mL | 9.1141 mL | 18.2282 mL | 45.5705 mL |
| 5 mM | 0.3646 mL | 1.8228 mL | 3.6456 mL | 9.1141 mL | |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8228 mL | 4.5571 mL | |
| 15 mM | 0.1215 mL | 0.6076 mL | 1.2152 mL | 3.0380 mL | |
| 20 mM | 0.0911 mL | 0.4557 mL | 0.9114 mL | 2.2785 mL | |
| 25 mM | 0.0729 mL | 0.3646 mL | 0.7291 mL | 1.8228 mL | |
| 30 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5190 mL | |
| 40 mM | 0.0456 mL | 0.2279 mL | 0.4557 mL | 1.1393 mL | |
| 50 mM | 0.0365 mL | 0.1823 mL | 0.3646 mL | 0.9114 mL | |
| 60 mM | 0.0304 mL | 0.1519 mL | 0.3038 mL | 0.7595 mL | |
| 80 mM | 0.0228 mL | 0.1139 mL | 0.2279 mL | 0.5696 mL | |
| 100 mM | 0.0182 mL | 0.0911 mL | 0.1823 mL | 0.4557 mL |