| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
Sipagladenant (oral; 0.3 mg/kg; once) therapy improves cognitive impairment caused by decreased dopamine function in the medial prefrontal cortex [2]. Treatment with cisparadenam (oral; 0.1 mg/kg; once) improves alternating behavior [2]. Treatment with cisparadenam (oral; 0.1 mg/kg; once) improves gait metrics [2].
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| Animal Protocol |
Animal/Disease Models: Medial prefrontal lobe dopaminergic terminal damage CD (SD) IGS male rat [2]
Doses: 0.3 mg/kg Route of Administration: Oral; Route of Administration: Oral. 0.3 mg/kg; primary Experimental Results: demonstrated longer exploration time for novel objects (65.03%) than for familiar objects (34.97%) (p<0.001). Animal/Disease Models: Cognitive impairment and/or movement disorder ICR mice [2] Doses: 0.1 mg/kg Route of Administration: Oral; 0.1 mg/kg; Experimental Results: Compared with the excipient administration group (59.6%), demonstrated Dramatically higher alternation behavior (69.5%) (p<0.01). Animal/Disease Models: Cognitive impairment and/or movement impairment ICR mice [2] Doses: 0.1 mg/kg Route of Administration: Oral; 0.1 mg/kg; Experimental Results: Compared with the vehicle administration group, the maximum left hind paw The contact area and gait area increased Dramatically (p<0.05), and the maximum contact area and gait area of the right front paw tended to become larger (p<0.1). |
| References |
[1]. https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl127.pdf?sfvrsn=8544ca1e_3&download=true
[2]. Horita, Takako. THERAPEUTIC AGENT FOR FRONTAL LOBE DYSFUNCTION, WO2016148308A1. |
| Additional Infomation |
KW-6356 is a selective antagonist of adenosine A2A receptors developed by Kyowa Kirin.
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| Molecular Formula |
C20H19N3O4S
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|---|---|
| Molecular Weight |
397.447563409805
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| Exact Mass |
397.109
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| CAS # |
858979-50-7
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| PubChem CID |
23144148
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
572
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(NC(C2C=NC(C)=CC=2)=O)=NC(C2=CC=CO2)=C1C(C1CCOCC1)=O
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| InChi Key |
KMFLQPJJHQNKKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N3O4S/c1-12-4-5-14(11-21-12)19(25)23-20-22-16(15-3-2-8-27-15)18(28-20)17(24)13-6-9-26-10-7-13/h2-5,8,11,13H,6-7,9-10H2,1H3,(H,22,23,25)
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| Chemical Name |
N-[4-(furan-2-yl)-5-(oxane-4-carbonyl)-1,3-thiazol-2-yl]-6-methylpyridine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~125.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5160 mL | 12.5802 mL | 25.1604 mL | |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0321 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 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.
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