PF-07054894 |
| Katalog-Nr.GC73182 |
PF-07054894 ist ein oral aktiver und potenter C-C Chemoattractant Cytokin (Chemokin)-Rezeptor 6 (CCR6)-Antagonist, der die CCR6-vermittelte Chemotaxie mit einem IC50-Wert von 5,7 nM in vitro blockiert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2413693-96-4
Sample solution is provided at 25 µL, 10mM.
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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.
PF-07054894 (1-3000 nM, 1 h) inhibits CCL20/CCR6-mediated T Cell chemotaxis in an insurmountable manner[2].
PF-07054894 (10 mg/kg, p.o., twice a day for 6 consecutive days) increases circulating CCR6+ T cells in naïve cynomolgus monkeys[2][3].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].
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.
[3]. Li W, et al. A novel CCR6 antagonist (PF-07054894) that distinguishes between homologous chemokine receptors, increases basal circulating CCR6+ T cells, and ameliorates interleukin-23-induced skin inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2023. [4]. Chinigo G M, et al. Early Process Development of PF-07054894, a Squaramide-Based Antagonist of C–C Chemokine Receptor Type 6 (CCR6)[J]. Organic Process Research & Development, 2024.
| Cas No. | 2413693-96-4 | SDF | |
| Formula | C24H30N6O4 | M.Wt | 466.53 |
| Löslichkeit | DMSO : 100 mg/mL (214.35 mM; Need ultrasonic) | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1435 mL | 10.7174 mL | 21.4348 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.287 mL |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1435 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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