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Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Upadacitinib [1310726-60-3]

Imprimer

Référence HY-19569-5mg

Conditionnement : 5mg

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Description

Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC₅₀=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research^[1]^[2].

IC₅₀ & Target^[1]

JAK1

0.043 μM (IC₅₀)

JAK2

0.2 μM (IC₅₀)

JAK3

2.3 μM (IC₅₀)

Tyk2

4.7 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Sf21	IC₅₀	120 nM Compound: 6	Inhibition of recombinant C-terminal His6-tagged human JAK2 kinase domain (808 to end residues) expressed in baculovirus-infected Sf21 cells in presence of 0.1 mM ATP Inhibition of recombinant C-terminal His6-tagged human JAK2 kinase domain (808 to end residues) expressed in baculovirus-infected Sf21 cells in presence of 0.1 mM ATP	[PMID: 31318208]
Sf9	IC₅₀	2304 nM Compound: 6	Inhibition of GST-fused recombinant human JAK3 catalytic domain (811-1103 residues) expressed in Sf9 cells in presence of 0.1 mM ATP Inhibition of GST-fused recombinant human JAK3 catalytic domain (811-1103 residues) expressed in Sf9 cells in presence of 0.1 mM ATP	[PMID: 31318208]
Sf9	IC₅₀	47 nM Compound: 6	Inhibition of GST-fused recombinant human JAK1 catalytic domain (845-1142 residues) expressed in Sf9 cells in presence of 0.1 mM ATP Inhibition of GST-fused recombinant human JAK1 catalytic domain (845-1142 residues) expressed in Sf9 cells in presence of 0.1 mM ATP	[PMID: 31318208]

In Vitro

In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance)^[1]. The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Lewis rats (Rat adjuvant-induced arthritis model)^[3]
Dosage:	0.1, 0.3, 1, 3, 10 mg/kg
Administration:	Oral gavage; twice a day for 10 days
Result:	Inhibited disease pathology in rat adjuvant induced arthritis.

Essai clinique

Masse moléculaire

380.37

Formule

C₁₇H₁₉F₃N₆O

CAS No.

1310726-60-3

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1C[C@@H](CC)[C@@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (262.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6290 mL	13.1451 mL	26.2902 mL
5 mM	0.5258 mL	2.6290 mL	5.2580 mL
10 mM	0.2629 mL	1.3145 mL	2.6290 mL

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (7.23 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (7.23 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.55 mg/mL (1.45 mM); Clear solution

Pureté et documentation

Purity: 99.98%

Fiche technique (280 KB) SDS (393 KB)

COA (255 KB) HNMR (257 KB) RP-HPLC (253 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. [Content Brief]

[2]. J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823.

[3]. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23. [Content Brief]

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Référence HY-19569-5mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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