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JANEX-1

Cat. No. M5028
JANEX-1 Structure
Synonym:

WHI-P131

Size Price Availability Quantity
10mM*1mL USD 110  USD110 In stock
5mg USD 100  USD100 In stock
10mg USD 180  USD180 In stock
50mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

The incidence of diabetes at 25 weeks was only 9% for NOD females treated with daily injections of JANEX-1 (100 mg/kg/day) from Week 10 through Week 25 (P = 0.007). Furthermore, JANEX-1 prevented the development of insulitis and diabetes in NOD-scid/scid females after adoptive transfer of splenocytes from diabetic NOD females.The antigen-induced degranulation and activation of MAPKs were inhibited by WHI-P131 and WHI-P154 in both groups of BMMCs, indicating that these compounds inhibit a certain step except for Jak3. The antigen-induced increase in the activity of Fyn, a probable tyrosine kinase of Gab2, was also inhibited by WHI-P131 and WHI-P154 in RBL-2H3 cells.

Customer Product Validations & Biological Datas
Source PLoS One (2016). Figure 1. JANEX-1
Method flow cytometry
Cell Lines human blood T lymphocytes
Concentrations 80 μM
Incubation Time 5, 24 or 48 h
Results Both PP2 and WHI-P131decreased the number of CD25+ cells in PHA-induced cultures, reduced the S-phase induction and suppressed the growth of activated PBL
Chemical Information
Molecular Weight 297.31
Formula C16H15N3O3
CAS Number 202475-60-3
Solubility (25°C) DMSO:~1 mg/ml
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Linwong W,et.al. Br J Pharmacol. Inhibition of the antigen-induced activation of rodent mast cells by putative Janus kinase 3 inhibitors WHI-P131 and WHI-P154 in a Janus kinase 3-independent manner.

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Keywords: JANEX-1, WHI-P131 supplier, JAK, inhibitors, activators


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