| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vivo |
AS2444697 was efficacious in rat adjuvant-induced arthritis (ED50 2.7 mg/kg, BID, PO) and rat collagen-induced arthritis (ED50 1.6 mg/kg, BID, PO) disease models. Pharmacokinetic investigations in rats (F% 50) and dogs (F% 78) indicated high bioavailability [1]. AS2444697 (0.3-3 mg/kg) significantly elevated the levels of IL-1β, IL-6, TNF-α, MCP-1 and aminotransferases (ALT and AST) in the plasma of LPS/GalN-treated mice. A single injection of AS2444697 (0.3-3 mg/kg) dose-dependently decreases plasma levels of all parameters, and these effects are significant at doses of 1 mg/kg or higher [2]. After oral administration of AS2444697 (3 mg/kg) to 5/6 Nx rats, the concentration of the original drug in plasma and tissues (liver and kidney) reached a peak at 1 hour, and subsequently steadily dropped, with a terminal half-life of 2.7-2.9 hours [2].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Male 6weeks old Wistar rats and balb/c (Bagg ALBino) mouse [2]
Doses: 0.3-3 mg/kg Route of Administration: single dose; oral Experimental Results: plasma IL-1β, IL-6, TNF- Alpha, MCP-1, and transaminases (ALT and AST) levels were Dramatically elevated. |
| References |
|
| Molecular Formula |
C19H21CLN6O4
|
|---|---|
| Molecular Weight |
432.860842466354
|
| Exact Mass |
432.131
|
| Elemental Analysis |
C, 52.72; H, 4.89; Cl, 8.19; N, 19.42; O, 14.78
|
| CAS # |
1287665-60-4
|
| Related CAS # |
1287665-60-4 (HCl);1287665-58-0;
|
| PubChem CID |
118719434
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
|
| Complexity |
601
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.O1CCC(CC1)N1C=C(C(C(N)=O)=N1)NC(C1=COC(C2C=CN=C(C)C=2)=N1)=O
|
| InChi Key |
FGNHLIIFEDYNFZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H20N6O4.ClH/c1-11-8-12(2-5-21-11)19-23-15(10-29-19)18(27)22-14-9-25(24-16(14)17(20)26)13-3-6-28-7-4-13;/h2,5,8-10,13H,3-4,6-7H2,1H3,(H2,20,26)(H,22,27);1H
|
| Chemical Name |
N-[3-carbamoyl-1-(oxan-4-yl)pyrazol-4-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide;hydrochloride
|
| Synonyms |
AS-2444697; AS 2444697; AS2444697; AS-2444697 HCl; AS-2444697 hydrochloride.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 12.5 mg/mL (~28.88 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.86 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3102 mL | 11.5511 mL | 23.1022 mL | |
| 5 mM | 0.4620 mL | 2.3102 mL | 4.6204 mL | |
| 10 mM | 0.2310 mL | 1.1551 mL | 2.3102 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
