PF-07054894
Based on 1 Customer Validation
PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.
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- Purity: 99.15%
- CAS No.: 2413693-96-4
- 화학식: C24H30N6O4
- 분자량:466.53
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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)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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CCR6 |
PF-07054894 (1-3000 nM, 1 h) inhibits CCL20/CCR6-mediated T Cell chemotaxis in an insurmountable manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-07054894 (100 mg/kg, p.o., once or twice per day for 12 days) is efficacious in interleukin-23-induced inflammation in skin inflammation mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:10 mg/kg
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Administration:p.o., twice a day for 6 consecutive days
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Result:Resulted in an increase in the frequency of most circulating CCR6+ T lymphocytes populations examined (CCR6+ CD4+ and CD8+ cells including total, effector, memory, Th17, and Th1/17 cells).
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Animal Model:Skin inflammation mouse model[2]
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Dosage:100 mg/kg
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Administration:p.o., once or twice per day for 12 days
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Result:Inhibited mouse ear swelling induced by interleukin-23 intradermal injection.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2413693-96-4
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Appearance Solid
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분자량 466.53
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화학식 C24H30N6O4
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Color Light yellow to yellow
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SMILES
OC1=C(C(N(C)C)=O)N=CC=C1NC2=C(N[C@@H](C3=NN(C)C=C3C)C4(C)CCCC4)C(C2=O)=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 (214.35 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 (5.36 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 (5.36 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 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 (278 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
[1]. Gómez S, et, al. Desarrollo de anticuerpos terapéuticos contra el receptor CCR6 humano.
[2]. Li W, et al. A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6+ T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation. J Pharmacol Exp Ther. 2023 Jul;386(1):80-92. [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 (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 |
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| DMSO | 1 mM | 2.1435 mL | 10.7174 mL | 21.4348 mL | 53.5871 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.2870 mL | 10.7174 mL | |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1435 mL | 5.3587 mL | |
| 15 mM | 0.1429 mL | 0.7145 mL | 1.4290 mL | 3.5725 mL | |
| 20 mM | 0.1072 mL | 0.5359 mL | 1.0717 mL | 2.6794 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8574 mL | 2.1435 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7145 mL | 1.7862 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5359 mL | 1.3397 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4287 mL | 1.0717 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8931 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2679 mL | 0.6698 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2143 mL | 0.5359 mL |
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