iJak-381 (Synonyms: iJak381; iJak 381; iJak-381; GDC-0214; GDC 0214; GDC0214;) |
Catalog No.GB62277
One-Click Copy Product Info
|
iJAK-381 is a novel, small-molecule inhibitor selectively targeting the Janus kinase (JAK) family, including JAK1, JAK2, JAK3 and TYK with IC50 values of 8.52, 53.4, 5998 and 240nM respectively at 1mM ATP.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1831144-46-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
iJAK-381 is a novel, small-molecule inhibitor selectively targeting the Janus kinase (JAK) family, including JAK1, JAK2, JAK3 and TYK with IC50 values of 8.52, 53.4, 5998 and 240nM respectively at 1mM ATP[1]. In preclinical species, iJAK-381 is retained in the lung and is rapidly cleared in the circulation[2].
In vivo, iJak-381 (10.7mg/kg) administered via dry powder inhalation in Ovalbumin-induced asthma mice model reduced total BAL cells, eosinophils, and expression of IL-13-dependent genes also inhibited pSTAT6 and pSTAT3 induction[1]. Thin film freezing (TFF)-iJak-381 powders (0.5mg/kg) were delivered via intratracheal administration into each Sprague−Dawley rat with a single dose. Four formulations of TFF-iJak-381 were tested: F20 (80% iJak-381, 20% lactose), F21 (80% iJak-381, 20% leucine), F22 (80% iJak-381, 10% lactose, 10% leucine), and micronized iJak-381 blended with micronized leucine. The formulation F20, which contains 80% iJak-381 and 20% lactose, provided enhanced lung targeting with reduced systemic exposure compared to micronized iJak-381[3].
References:
[1] Dengler H S, X M, Peng I, et al. Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma. Sci Transl Med. 2018 Nov 21;10(468):eaao2151.
[2] Braithwaite I E, Cai F, Tom J A, et al. Inhaled JAK inhibitor GDC-0214 reduces exhaled nitric oxide in patients with mild asthma: A randomized, controlled, proof-of-activity trial. J Allergy Clin Immunol. 2021 Sep;148(3):783-789.
[3] Moon C, Sahakijpijarn S, Maier E Y, et al. Inhaled JAK Inhibitor GDC-0214 Nanoaggregate Powder Exhibits Improved Pharmacokinetic Profile in Rats Compared to the Micronized Form: Benefits of Thin Film Freezing. Mol Pharm. 2024 Feb 5;21(2):564-580.
| Animal experiment [1]: | |
|
Animal models |
Guinea pigs |
|
Preparation Method |
Guinea pigs were immunized twice with OVA (day 0 and 7). On day 28, animals received a single OVA challenge. One hour before the OVA challenge, animals received either air or iJak-381 (1.3 and 6.2mpk) at the indicated dose via dry powder in halation (DPI) system. Twenty-four hours after the final challenge, lungs, spleens, and plasma were collected. |
|
Dosage form |
1.3 and 6.2mpk; DPI; day 0, 7 and 28 |
|
Applications |
DPI iJak-381 administration resulted in a dose dependent reduction of inflammation, with very few remaining tissue infiltrates. The lung-restricted exposure of iJak-381 in guinea pigs was observed. |
|
References: |
|
| Cas No. | 1831144-46-7 | SDF | |
| Synonyms | iJak381; iJak 381; iJak-381; GDC-0214; GDC 0214; GDC0214; | ||
| Canonical SMILES | O=C(C1=C2N=CC=CN2N=C1)NC3=CN(CC(N4CCC(N(CCC#N)C)CC4)=O)N=C3C5=CC(Cl)=CC=C5OC(F)F | ||
| Formula | C28H28ClF2N9O3 | M.Wt | 612.0388 |
| Solubility | Soluble in DMSO | Storage | Store at-20℃ |
| 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 | 1.6339 mL | 8.1694 mL | 16.3388 mL |
| 5 mM | 326.8 μL | 1.6339 mL | 3.2678 mL |
| 10 mM | 163.4 μL | 816.9 μL | 1.6339 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)