Synonym
Sipagladenant; SCHEMBL879438; EX-A7778; KW-6356
IUPAC/Chemical Name
N-[4-(furan-2-yl)-5-(oxane-4-carbonyl)-1,3-thiazol-2-yl]-6-methylpyridine-3-carboxamide
InChi Key
KMFLQPJJHQNKKF-UHFFFAOYSA-N
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)
SMILES Code
O=C(C1=CC=C(C)N=C1)NC2=NC(C3=CC=CO3)=C(C(C4CCOCC4)=O)S2
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
397.45
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Ohno Y, Suzuki M, Asada H, Kanda T, Saki M, Miyagi H, Yasunaga M, Suno C,
Iwata S, Saito JI, Uchida S. In Vitro Pharmacological Profile of KW-6356, a
Novel Adenosine A2A Receptor Antagonist/Inverse Agonist. Mol
Pharmacol. 2023 Jun;103(6):311-324. doi: 10.1124/molpharm.122.000633. Epub 2023
Mar 9. PMID: 36894319.
2: Maeda T, Kimura T, Sugiyama K, Yamada K, Hiraiwa R, Nishi M, Hattori N;
6356-002 study group. Randomized controlled trial of KW-6356 monotherapy in
patients with early untreated Parkinson's disease. Parkinsonism Relat Disord.
2023 Dec;117:105907. doi: 10.1016/j.parkreldis.2023.105907. Epub 2023 Oct 31.
PMID: 37948832.
3: Tayama T, Ishiuchi M, Sugiyama K, Oka Y, Maeda H, Nagata Y, Hruska M, Kagawa
Y. Safety, Tolerability, and Pharmacokinetics of the Novel Adenosine
A2A Antagonist/Inverse Agonist KW-6356 Following Single and Multiple
Oral Administration in Healthy Volunteers. Clin Pharmacol Drug Dev. 2023
Aug;12(8):801-809. doi: 10.1002/cpdd.1222. Epub 2023 Jan 22. PMID: 36683291.
4: Ohno Y, Okita E, Kawai-Uchida M, Shoukei Y, Soshiroda K, Kanda T, Uchida S.
The adenosine A2A receptor antagonist/inverse agonist, KW-6356
enhances the anti-parkinsonian activity of L-DOPA with a low risk of dyskinesia
in MPTP-treated common marmosets. J Pharmacol Sci. 2023 Jul;152(3):193-199. doi:
10.1016/j.jphs.2023.05.001. Epub 2023 May 11. PMID: 37257947.
5: Ohno Y, Okita E, Kawai-Uchida M, Fukuda N, Shoukei Y, Soshiroda K, Yamada K,
Kanda T, Uchida S. Anti-parkinsonian activity of the adenosine A2A
receptor antagonist/inverse agonist KW-6356 as monotherapy in MPTP-treated
common marmosets. Eur J Pharmacol. 2023 Jul 5;950:175773. doi:
10.1016/j.ejphar.2023.175773. Epub 2023 May 3. PMID: 37146707.
