BTK inhibitor 18 |
| رقم الكتالوجGC64360 |
مثبط BTK 18 هو مثبط Btk قوي وانتقائي وفعال عن طريق الفم وتساهمي مع IC50 من 142 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities[1].
BTK inhibitor 18 (Compound 27) irreversibly inhibits BTK by targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation[1].BTK inhibitor 18 (Compound 27) inhibits anti-IgM-induced activation of B cells in human whole blood with an IC50 of 84 nM[1]. BTK inhibitor 18 (Compound 27) also inhibits BMX, LCK, ErbB4, TEC, and TXK kinases with IC50 values of 129 nM, 130 nM, 377 nM, 409 nM, 1770 nM, respectively[1].
BTK inhibitor 18 (Compound 27; 1-30 mg/kg; oral administration; once a day; for 7 days) treatment shows dose-dependent efficacy at reducing joint inflammation in a rat collagen-induced arthritis model[1].The IV and PO pharmacokinetics of BTK inhibitor 18 (Compound 27) are investigated in nonfasted rats (1 and 5 mg/kg IV and PO) and fasted dogs (0.5 and 2.5 mg/kg IV and PO). IV pharmacokinetics are characterized by moderate clearance in rat and low clearance in dog, a moderate volume of distribution, and a short plasma half-life across both species (T1/2 of 0.3 h and 1.9 h for rat and dog, respectively). The oral bioavailability is 30% and 68% in rat and dog, respectively[1].
[1]. Mark S Tichenor, et al. Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity. ACS Med Chem Lett. 2021 Apr 5;12(5):782-790.
| Cas No. | SDF | ||
| Formula | C29H25N5O4S2 | M.Wt | 571.67 |
| الذوبان | Storage | Store at -20°C | |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7493 mL | 8.7463 mL | 17.4926 mL |
| 5 mM | 0.3499 mL | 1.7493 mL | 3.4985 mL |
| 10 mM | 0.1749 mL | 0.8746 mL | 1.7493 mL |
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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