CAS 540737-29-9 Tofacitinib Citrate - Analytical Products / Alfa Chemistry

CAT	APS540737299
CAS	540737-29-9
Structure
MDL Number	MFCD11616529
Synonyms	(3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile 2-Hydroxy-1,2,3-propanetricarboxylate (1:1), CP 690500-10, Tasocitinib citrate, Xeljanz, 3-Piperidinamine, 1-(cyanoacetyl)-4-methyl-N-methyl-N-1H-pyrrolo[2,3-d]pyrimidin-4-yl-, (3R,4R)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (9CI), CP 690550-10, Tofacitinib citrate
IUPAC Name	2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
Molecular Weight	504.49
Molecular Formula	C16H20N6O.C6H8O7
Canonical SMILES	C[C@@H]1CCN(C[C@@H]1N(C)c2ncnc3[nH]ccc23)C(=O)CC#N.OC(=O)CC(O)(CC(=O)O)C(=O)O
InChI	InChI=1S/C16H20N6O.C6H8O7/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16
InChI Key	SYIKUFDOYJFGBQ-YLAFAASESA-N

Description	≥98% (HPLC)
Solubility	DMSO: 5 mg/mL (clear solution; warmed)
Accurate Mass	504.1969
API Family	Matrix - API Family Tofacitinib Citrate
Assay	≥98% (HPLC)
Color	white to beige
Form	powder
Format	Neat
Shipping	Room Temperature
Size	250MG
Storage Conditions	+5°C
Subcategory	API standards, Immunosuppressants, Mikromol
Type	API

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Case Study

Preparation of Solid Lipid Nanoparticles Loaded with N-Trimethyl Chitosan and Tofacitinib Citrate

Roy, Harekrishna, et al. Journal of Drug Delivery Science and Technology 87 (2023): 104789.

In recent years, solid lipid nanoparticles (SLN) have emerged as a promising dosage form innovation. To enhance skin permeability, SLNs loaded with tofacitinib citrate (TFC) were developed.
First, tripalmitin (TP) was gently stirred in porcelain to melt and form the lipid phase. TFC was dispersed in distilled water in a separate beaker with an appropriate amount of Brij-35. The drug dispersion was then introduced into the lipid phase and thoroughly mixed using a magnetic stirrer while maintaining a temperature of 70 °C. In another beaker, N-Trimethyl Chitosan (NTC) solutions of different concentrations were prepared, keeping the temperature at 70 °C. To create a hot o/w microemulsion, the lipid phase was poured into the aqueous phase and continuously mixed in a mechanical stirrer. Finally, the hot microemulsion was dispersed in cold water (2-5 °C) for 1 hour while being stirred continuously on a magnetic stirrer at suitable RPM according to the Box-Behnken Design (BBD), resulting in solid lipid nanoparticles (SLN). To stabilize the prepared lipid nanoparticles, the dispersion was further ultrasonicated at 30% amplitude using a probe-type ultrasonic generator for 30 minutes. The final volume was obtained by adding the required amount of distilled water to reach 100 mL.

Preparation of Citrate Tofacitinib Liposomes for Effective Treatment of Rheumatoid Arthritis

Shen, Qiying, et al. Die Pharmazie-An International Journal of Pharmaceutical Sciences 75.4 (2020): 131-135.

The low drug concentration at the target site and adverse systemic side effects are major obstacles to the effective treatment of rheumatoid arthritis (RA). To enhance the efficacy of citrate tofacitinib (TOF), a liposome system was developed for targeted delivery to inflamed joints.
The preparation of citrate tofacitinib liposomes (TOFL) involves two steps: the formation of blank liposomes (blank-L) and drug-loaded liposomes. First, blank liposomes were prepared using a thin film hydration method. Cholesterol (50 mg) and SPC (100 mg) were dissolved in ethanol and then dried under reduced pressure at 50 °C for about 30 minutes using a rotary evaporator. Next, 2 mL of C₆H₈O₇-C₇H₅O₃Na (pH 3.6) was added to the dried mixture as an internal buffer for hydration in a vortex mixer. The liposome dispersion was then sonicated in an ice bath for 20 minutes and filtered through a 0.22 μm filter membrane to achieve uniform size of the blank liposomes.
Subsequently, the TOF was loaded into the liposomes using a pH gradient method. The external pH of the liposomes was adjusted to pH 8 using Na₂CO₃, and the liposomes were mixed with a TOF solution (4 mg). Finally, this mixture was incubated at 60 °C for 10 minutes with occasional shaking, and free TOF was removed by ultrafiltration.